Author: "Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)" - Searchworks@Jio Institute Digital Library Search Results

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717 results on '"Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)"'

1. Physico-chemical role of CdSe/ZnS quantum dots in the photo-polymerization process of acrylate composite materials

Author: Barichard, Anne, Galstian, Tigran, Israëli, Yaël, Photochimie, Institut de Chimie de Clermont-Ferrand (ICCF), Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Center of Optics, Photonics and Laser, Université Laval [Québec] (ULaval)-Université Laval [Québec] (ULaval), Center of Optics, Photonics and Laser, Université Laval [Québec] (ULaval), Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Center of Optics, Photonics and Laser, Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Bonnefoy, Stéphanie
Subjects: technology, industry, and agriculture, equipment and supplies
Abstract: International audience; The work presented in this paper is devoted to the physico-chemical role of quantum dots (QDs) in the photopolymerization of composite materials. We show first that the photoexcitation of CdSe/ZnS semiconductor quantum dots can initiate the polymerization of an acrylate monomer in association with a tertiary amine and in the absence of a photoinitiator. But by using a holographic technique, among the others, the gratings recorded in such composite materials are not stable and relax once the light interference pattern is switched off. This behaviour is attributed to a very low degree of conversion of monomers, which does not prevent the post-exposure diffusion of monomers and nanoparticles. The comparison with gratings obtained in the presence of a photosensitizer dye (higher hologram quality and stability) highlights the key importance of using such dye in the polymerization process. The gratings recorded in the complete syrup, containing the dye and QDs which differ by their size and UV-visible absorption spectra, exhibit an additional refractive index modulation. The latter results from the spatial distribution of QDs and the change in the kinetics of polymerization. We further focus on understanding the fall of the polymerization rate owing to the presence of QDs. This decrease may result from the trapping of the tertiary amine (co-initiator) at the surface of those QDs, which reduces the rate of decay of the dye and, consequently, the polymerization rate. Under such conditions, the diffusion of QDs and monomers is favoured and their spatial redistribution is enhanced. These features contribute to modify the physical properties of the gratings.
Published: 2012

2. P-gp expression levels in the erythrocytes of brown trout: a new tool for aquatic sentinel biomarker development

Author: Emeline Valton, Marie-Laure Bayle, Bruno Combourieu, Christian Amblard, Ivan Wawrzyniak, Mahchid Bamdad, François Desmolles, Frédérique Penault-Llorca, Fabrice Kwiatkowski, Laboratoire Microorganismes : Génome et Environnement (LMGE), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Université d'Auvergne - Clermont-Ferrand I (UdA)-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Service Central d'Analyse (SCA), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), service de recherche clinique, Centre Jean Perrin [Clermont-Ferrand] (UNICANCER/CJP), UNICANCER-UNICANCER, UNICANCER, Imagerie Moléculaire et Stratégies Théranostiques (IMoST), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020]), Laboratoire Biochimie Médicale (UMR 384), Institut National de la Santé et de la Recherche Médicale (INSERM), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Université d'Auvergne - Clermont-Ferrand I (UdA), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: 0301 basic medicine, Trout, Health, Toxicology and Mutagenesis, Clinical Biochemistry, Gene Expression, [SDV.CAN]Life Sciences [q-bio]/Cancer, 010501 environmental sciences, Biology, 01 natural sciences, Biochemistry, 03 medical and health sciences, chemistry.chemical_compound, Brown trout, brown trout, Rivers, Detoxification, Water Pollution, Chemical, Animals, ATP Binding Cassette Transporter, Subfamily B, Member 1, Polycyclic Aromatic Hydrocarbons, 0105 earth and related environmental sciences, Pesticide Residues, river pollution, Biomarker, Blood, 030104 developmental biology, chemistry, 13. Climate action, Cell culture, Environmental chemistry, erythrocytes, P-gp, biomarker, Xenobiotic, River pollution, Biomarkers, Environmental Monitoring
Abstract: P-glycoprotein (P-gp) is a ubiquitous membrane detoxification pump involved in cellular defence against xenobiotics. Blood is a hub for the trade and transport of physiological molecules and xenobiotics. Our recent studies have highlighted the expression of a 140-kDa P-gp in brown trout erythrocytes in primary cell culture and its dose-dependent response to Benzo[a]pyrene pollutant.The purpose of this study was focused on using P-gp expression in brown trout erythrocytes as a biomarker for detecting the degree of river pollution.abcb1 gene and P-gp expression level were analysed by reverse transcriptase-PCR and Western blot, in the erythrocytes of brown trouts. The latter were collected in upstream and downstream of four rivers in which 17 polycyclic aromatic hydrocarbons and 348 varieties of pesticides micro-residues were analysed by liquid chromatography and mass spectrometry.The abcb1 gene and the 140-kDa P-gp were not expressed in trout erythrocytes from uncontaminated river. In contrast, they are clearly expressed in contaminated rivers, in correlation with the river pollution degree and the nature of the pollutants.This biological tool may offer considerable advantages since it provides an effective response to the increasing need for an early biomarker.
Published: 2017

3. Production of heparin and λ-carrageenan anti-heparanase derivatives using a combination of physicochemical depolymerization and glycol splitting

Author: Ingrid Fruitier-Arnaudin, Nicolas Bridiau, Hugo Groult, Frédéric Sannier, Nicolas Poupard, Jean-Marie Piot, Thierry Maugard, Stéphanie Bordenave-Juchereau, Justine Bodin, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), LIttoral ENvironnement et Sociétés (LIENSs), La Rochelle Université (ULR)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Génie Protéique et Cellulaire (LGPC), La Rochelle Université (ULR), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), LIttoral ENvironnement et Sociétés - UMRi 7266 (LIENSs), Université de La Rochelle (ULR)-Centre National de la Recherche Scientifique (CNRS), and Université de La Rochelle (ULR)
Subjects: 0301 basic medicine, Polymers and Plastics, Carrageenan, Glycols, 03 medical and health sciences, Hydrolysis, chemistry.chemical_compound, Sulfation, Materials Chemistry, medicine, [SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology, Heparanase, [SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biochemistry [q-bio.BM], IC50, ComputingMilieux_MISCELLANEOUS, Glucuronidase, chemistry.chemical_classification, Heparin, Depolymerization, Organic Chemistry, 030104 developmental biology, Enzyme, Biochemistry, chemistry, medicine.drug
Abstract: Strongly associated with tumor angiogenesis and metastasis, the enzyme heparanase is an endo-β-d-glucuronidase which is overexpressed in the tumor microenvironment. Its inhibition could be one of the most promising anti-angiogenic approaches to date. Although heparin is known as a good heparanase inhibitor, it also possesses major anticoagulant properties that may be incompatible with its use as an anti-angiogenic agent, hence the considerable interest for other sources of sulfated polysaccharides. Recent investigations point to λ-carrageenans, highly sulfated galactans with a tremendous potential that are found in red algae. This study describes the production of low-molecular-weight (LMW) heparins and λ-carrageenans, using a combination of glycol splitting and ultrasonically-assisted radical hydrolysis using hydrogen-peroxide. The structural characteristics, as well as the anticoagulant and antiheparanase activities of the resulting products were assessed. The best candidate was a LMW glycol-split λ-carrageenan that displayed major anti-heparanase properties, with an IC50 of 7.32ng/mL and a close-to-zero anticoagulant activity.
Published: 2017

4. Structure and dynamics of G protein-coupled receptor–bound ghrelin reveal the critical role of the octanoyl chain

Author: Pascal Demange, Maxime Louet, Alain Milon, Jacky Marie, Guillaume Ferré, Georges Czaplicki, Jean-Louis Banères, Pedro Renault, Laurent Gavara, Nicolas Floquet, Céline M'Kadmi, Sonia Cantel, Jean-Alain Fehrentz, Bartholomé Delort, Oliver Saurel, Marjorie Damian, Laboratoire de l'intégration, du matériau au système (IMS), Université Sciences et Technologies - Bordeaux 1-Institut Polytechnique de Bordeaux-Centre National de la Recherche Scientifique (CNRS), Molécules Thérapeutiques in silico (MTI), Université Paris Diderot - Paris 7 (UPD7)-Institut National de la Santé et de la Recherche Médicale (INSERM), Institut de pharmacologie et de biologie structurale (IPBS), Centre National de la Recherche Scientifique (CNRS)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées, Institut de biologie physico-chimique (IBPC (FR_550)), Centre National de la Recherche Scientifique (CNRS), Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Groupe de recherche et d'analyse du social et de la sociabilité (GRASS), Université Paris 8 Vincennes-Saint-Denis (UP8)-Centre National de la Recherche Scientifique (CNRS), Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS), Université Sciences et Technologies - Bordeaux 1 (UB)-Institut Polytechnique de Bordeaux-Centre National de la Recherche Scientifique (CNRS), Université de Toulouse (UT)-Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and ANR-17-CE11-0011,allosig,allostérie, dynamique conformationnelle et signalisation via les RCPG(2017)
Subjects: Models, Molecular, 0301 basic medicine, Agonist, Conformational change, Magnetic Resonance Spectroscopy, Molecular model, Protein Conformation, medicine.drug_class, Acylation, [SDV]Life Sciences [q-bio], Growth hormone secretagogue receptor, Peptide, 010402 general chemistry, 01 natural sciences, Receptors, G-Protein-Coupled, Structure-Activity Relationship, 03 medical and health sciences, medicine, Animals, Humans, [SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology, Receptor, ComputingMilieux_MISCELLANEOUS, G protein-coupled receptor, chemistry.chemical_classification, Binding Sites, Multidisciplinary, digestive, oral, and skin physiology, Biological Sciences, Ghrelin, 0104 chemical sciences, [SDV.BBM.BP]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biophysics, 030104 developmental biology, chemistry, Biophysics, hormones, hormone substitutes, and hormone antagonists, Protein Binding, Signal Transduction
Abstract: Ghrelin plays a central role in controlling major biological processes. As for other G protein-coupled receptor (GPCR) peptide agonists, the structure and dynamics of ghrelin bound to its receptor remain obscure. Using a combination of solution-state NMR and molecular modeling, we demonstrate that binding to the growth hormone secretagogue receptor is accompanied by a conformational change in ghrelin that structures its central region, involving the formation of a well-defined hydrophobic core. By comparing its acylated and nonacylated forms, we conclude that the ghrelin octanoyl chain is essential to form the hydrophobic core and promote access of ghrelin to the receptor ligand-binding pocket. The combination of coarse-grained molecular dynamics studies and NMR should prove useful in improving our mechanistic understanding of the complex conformational space explored by a natural peptide agonist when binding to its GPCR. Such information should also facilitate the design of new ghrelin receptor-selective drugs.
Published: 2019

5. Preliminary results from the FARCE 2015 campaign: multidisciplinary study of the forest–gas–aerosol–cloud system on the tropical island of La Réunion

Author: Duflot, Valentin, Tulet, Pierre, Flores, Olivier, Barthe, Christelle, Colomb, Aurélie, Deguillaume, Laurent, Vaitilingom, Mickaël, Perring, Anne, Huffman, Alex, Hernandez, Mark, Sellegri, Karine, Robinson, Ellis, O'Connor, David, Gomez, Odessa, Burnet, Frédéric, Bourrianne, Thierry, Strasberg, Dominique, Rocco, Manon, Bertram, Allan, Chazette, Patrick, Totems, Julien, Fournel, Jacques, Stamenoff, Pierre, Metzger, Jean-Marc, Chabasset, Mathilde, Rousseau, Clothilde, Bourrianne, Eric, Sancelme, Martine, Delort, Anne-Marie, Wegener, Rachel, Chou, Cedric, Elizondo, Pablo, Laboratoire de l'Atmosphère et des Cyclones (LACy), Météo France-Université de La Réunion (UR)-Centre National de la Recherche Scientifique (CNRS), Peuplements végétaux et bioagresseurs en milieu tropical (UMR PVBMT), Institut de Recherche pour le Développement (IRD)-Centre de Coopération Internationale en Recherche Agronomique pour le Développement (Cirad)-Université de La Réunion (UR)-Institut National de la Recherche Agronomique (INRA), Laboratoire de météorologie physique (LaMP), Centre National de la Recherche Scientifique (CNRS)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Météorologie Physique - Clermont Auvergne (LaMP), Institut national des sciences de l'Univers (INSU - CNRS)-Université Clermont Auvergne (UCA)-Centre National de la Recherche Scientifique (CNRS), University of Wisconsin-Madison, Centre national de recherches météorologiques (CNRM), Météo France-Centre National de la Recherche Scientifique (CNRS), Department of Chemistry [Vancouver], University of British Columbia (UBC), Laboratoire des Sciences du Climat et de l'Environnement [Gif-sur-Yvette] (LSCE), Université Paris-Saclay-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université de Versailles Saint-Quentin-en-Yvelines (UVSQ)-Centre National de la Recherche Scientifique (CNRS), Sigma CLERMONT (Sigma CLERMONT), Institut national des sciences de l'Univers (INSU - CNRS)-Université de La Réunion (UR)-Centre National de la Recherche Scientifique (CNRS)-Météo-France, Centre de Coopération Internationale en Recherche Agronomique pour le Développement (Cirad)-Institut de Recherche pour le Développement (IRD)-Institut National de la Recherche Agronomique (INRA)-Université de La Réunion (UR), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Météorologie Physique (LaMP), Institut national des sciences de l'Univers (INSU - CNRS)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Institut national des sciences de l'Univers (INSU - CNRS)-Observatoire Midi-Pyrénées (OMP), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National d'Études Spatiales [Toulouse] (CNES)-Centre National de la Recherche Scientifique (CNRS)-Météo-France -Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National d'Études Spatiales [Toulouse] (CNES)-Centre National de la Recherche Scientifique (CNRS)-Météo-France -Centre National de la Recherche Scientifique (CNRS), Department of Chemistry [Vancouver] (UBC Chemistry), Université de Versailles Saint-Quentin-en-Yvelines (UVSQ)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS), Chimie Atmosphérique Expérimentale (CAE), Université de Versailles Saint-Quentin-en-Yvelines (UVSQ)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-Université de Versailles Saint-Quentin-en-Yvelines (UVSQ)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS), SIGMA Clermont (SIGMA Clermont), Centre National de la Recherche Scientifique (CNRS)-Université de La Réunion (UR)-Institut national des sciences de l'Univers (INSU - CNRS)-Météo France, Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut national des sciences de l'Univers (INSU - CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institut national des sciences de l'Univers (INSU - CNRS)-Météo France-Centre National de la Recherche Scientifique (CNRS), Institut national des sciences de l'Univers (INSU - CNRS)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université de Versailles Saint-Quentin-en-Yvelines (UVSQ), and Institut national des sciences de l'Univers (INSU - CNRS)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université de Versailles Saint-Quentin-en-Yvelines (UVSQ)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université de Versailles Saint-Quentin-en-Yvelines (UVSQ)
Subjects: [SDU.OCEAN]Sciences of the Universe [physics]/Ocean, Atmosphere, [SDU.STU.ME]Sciences of the Universe [physics]/Earth Sciences/Meteorology, [SDE.BE]Environmental Sciences/Biodiversity and Ecology
Abstract: International audience; The Forests gAses aeRosols Clouds Exploratory (FARCE) campaign was conducted in March-April 2015 on the tropical island of La Réunion. For the first time, several scientific teams from different disciplines collaborated to provide reference measurements and characterization of La Réunion vegetation, volatile organic compounds (VOCs), biogenic VOCs (BVOCs), (bio)aerosols and composition of clouds, with a strong focus on the Maïdo mountain slope area. The main observations obtained during this 2-month intensive field campaign are summarized. They include characterizations of forest structure, concentrations of VOCs and precursors emitted by forests, aerosol loading and optical properties in the planetary boundary layer (PBL), formation of new particles by nucleation of gas-phase precursors, ice-nucleating particles concentrations, and biological loading in both cloud-free and cloudy conditions. Simulations and measurements confirm that the Maïdo Observatory lies within the PBL from late morning to late evening and that, when in the PBL, the main primary sources impacting the Maïdo Observatory are of marine origin via the Indian Ocean and of bio-genic origin through the dense forest cover. They also show that (i) the marine source prevails less and less while reaching the observatory; (ii) when in the PBL, depending on the lo-calization of a horizontal wind shear, the Maïdo Observatory can be affected by air masses coming directly from the ocean and passing over the Maïdo mountain slope, or coming from inland; (iii) bio-aerosols can be observed in both cloud-free and cloudy conditions at the Maïdo Observatory; (iv) BVOC emissions by the forest covering the Maïdo mountain slope can be transported upslope within clouds and are a potential cause of secondary organic aerosol formation in the aqueous phase at the Maïdo Observatory; and (v) the simulation of dynamics parameters, emitted BVOCs and cloud life cycle in the Meso-NH model are realistic, and more advanced Meso-NH simulations should use an increased horizontal resolution (100 m) to better take into account the orography and improve the simulation of the wind shear front zone within which lies the Maïdo Observatory. Using various observations and simulations, this work draws up an inventory of the in situ studies that could be performed in La Réunion and at the Maïdo Observatory. It also aims to develop scientific collaborations and to support future scientific projects in order to better understand the forest-gas-aerosol-cloud system in an insular tropical environment.
Published: 2019

6. Developmental frontal brain activation differences in overcoming heuristic bias

Author: Wim De Neys, François Orliac, Grégoire Borst, Nicolas Poirel, Grégory Simon, Olivier Houdé, Katell Mevel, Olivier Etard, Neuropsychologie cognitive et neuroanatomie fonctionnelles de la mémoire humaine, Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU)-École Pratique des Hautes Études (EPHE), Université Paris sciences et lettres (PSL)-Université Paris sciences et lettres (PSL)-Institut National de la Santé et de la Recherche Médicale (INSERM), Laboratoire de psychologie du développement et de l'éducation de l'enfant (LaPsyDÉ - UMR 8240), Normandie Université (NU)-Normandie Université (NU)-Université Paris Descartes - Paris 5 (UPD5)-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Imagerie et Stratégies Thérapeutiques de la Schizophrénie (ISTS), Normandie Université (NU)-Normandie Université (NU), Service des Explorations Fonctionnelles [CHU Caen], CHU Caen, Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN), Mobilités : Vieillissement, Pathologie, Santé (COMETE), Normandie Université (NU)-Normandie Université (NU)-Institut National de la Santé et de la Recherche Médicale (INSERM), Université Paris Descartes - Paris 5 (UPD5)-Centre National de la Recherche Scientifique (CNRS), ANR-16-CE28-0010,DIAGNOR,DIAGNOSTIQUER LES DIFFERENCES INDIVIDUELLES DANS LA DETECTION DU BIAIS AU COURS DU RAISONNEMENT(2016), Normandie Université (NU)-Normandie Université (NU)-École pratique des hautes études (EPHE), CCSD, Accord Elsevier, Institut National de la Santé et de la Recherche Médicale (INSERM)-École pratique des hautes études (EPHE), Université Paris sciences et lettres (PSL)-Université Paris sciences et lettres (PSL)-Université de Caen Normandie (UNICAEN), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: Adult, Male, Brain activation, Aging, Adolescent, Cognitive Neuroscience, Prefrontal Cortex, Experimental and Cognitive Psychology, Neuropsychological Tests, Gyrus Cinguli, 050105 experimental psychology, Conflict, Psychological, Young Adult, 03 medical and health sciences, [SCCO]Cognitive science, Cognition, 0302 clinical medicine, Age groups, Reaction Time, medicine, Heuristics, Humans, 0501 psychology and cognitive sciences, Problem Solving, Anterior cingulate cortex, ComputingMilieux_MISCELLANEOUS, Cued speech, Neural correlates of consciousness, Heuristic, [SCCO.NEUR]Cognitive science/Neuroscience, 05 social sciences, [SCCO.NEUR] Cognitive science/Neuroscience, [SCCO] Cognitive science, Correct response, Magnetic Resonance Imaging, Inhibition, Psychological, Neuropsychology and Physiological Psychology, medicine.anatomical_structure, [SCCO.PSYC] Cognitive science/Psychology, [SCCO.PSYC]Cognitive science/Psychology, Female, Psychology, 030217 neurology & neurosurgery, Cognitive psychology
Abstract: Since reasoning is often biased by intuitive heuristics, the development of sound reasoning has long been postulated to depend on successful bias monitoring and inhibition. The present fMRI study aimed to identify neural correlates of developmental changes in these processes. A group of adults and young adolescents were presented with ratio-bias problems in which an intuitively cued heuristic response could be incongruent (conflict item) or congruent (no-conflict item) with the correct response. Results showed that successfully avoiding biased responding on conflict items across both age groups was associated with increased activation in Anterior Cingulate Cortex (ACC) and the right Lateral Prefrontal Cortex (LPFC) regions of interest. Critically, the right LPFC activation decreased with age. Biased responding did not result in right LPFC or ACC modulation and failed to show any developmental activation changes. We discuss implications for ongoing debates on the nature of heuristic bias and its development.
Published: 2019

7. Synthesis of aryl-thioglycopeptides through chemoselective Pd-catalyzed conjugation

Author: Vishwanatha, T.M., Montoir, D., Amoura, Mehdi, El Ababsa, Z., Yen-Pon, E., Robert, V., Beltramo, Massimiliano, Piller, V., Alami, M., Aucagne, V., Messaoudi, S., Frapart, Isabelle, Centre de biophysique moléculaire (CBM), Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institut de Chimie de Strasbourg, Université de Strasbourg (UNISTRA)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Physiologie de la reproduction et des comportements [Nouzilly] (PRC), Institut National de la Recherche Agronomique (INRA)-Institut Français du Cheval et de l'Equitation [Saumur]-Université de Tours-Centre National de la Recherche Scientifique (CNRS), Biomolécules : Conception, Isolement, Synthèse (BioCIS), Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Paris-Sud - Paris 11 (UP11)-Université de Cergy Pontoise (UCP), Université Paris-Seine-Université Paris-Seine, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Université Paris-Sud - Paris 11 (UP11)-Université de Cergy Pontoise (UCP), Université Paris-Seine-Université Paris-Seine-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Université de Strasbourg (UNISTRA)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Institut National de la Recherche Agronomique (INRA)-Institut Français du Cheval et de l'Equitation [Saumur] (IFCE)-Université de Tours (UT)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), ProdInra, Migration, Université Paris Saclay (COmUE), Univ Paris Saclay, Univ Paris Sud, CNRS, BioCIS, Chatenay Malabry, France, Partenaires INRAE, and Institut National de la Recherche Agronomique (INRA)-Institut Français du Cheval et de l'Equitation [Saumur]-Université de Tours (UT)-Centre National de la Recherche Scientifique (CNRS)
Subjects: [CHIM.ORGA]Chemical Sciences/Organic chemistry, [CHIM] Chemical Sciences, [CHIM]Chemical Sciences, [CHIM.ORGA] Chemical Sciences/Organic chemistry, ComputingMilieux_MISCELLANEOUS
Abstract: International audience
Published: 2019

8. Un outil de simulation : comprendre comment la sylviculture modifie la qualité génétique et les capacités d'adaptation des peuplements

Author: Francois Lefèvre, Godineau, C., Nicolas Beudez, François de Coligny, Francois Courbet, Oddou-Muratorio, S., Sanchez, L., Christine Deleuze, Christelle Pichot, Chartier, M., Musch, B., Francois, D., Girard, S., Guyot, J., Laurence Le-Legard Moreau, Philippe Riou-Nivert, Yves Rousselle, Aline Salvaudon, Sédilot-Gasmi, C., Unité de Recherches Forestières Méditerranéennes (URFM), Institut National de la Recherche Agronomique (INRA), Botanique et Modélisation de l'Architecture des Plantes et des Végétations (UMR AMAP), Centre National de la Recherche Scientifique (CNRS)-Université de Montpellier (UM)-Institut National de la Recherche Agronomique (INRA)-Centre de Coopération Internationale en Recherche Agronomique pour le Développement (Cirad)-Institut de Recherche pour le Développement (IRD [France-Sud]), Ecologie des Forêts Méditerranéennes (URFM), Unité de recherche Amélioration, Génétique et Physiologie Forestières (AGPF), Qualité des eaux et prévention des pollutions (UR QELY), Centre national du machinisme agricole, du génie rural, des eaux et forêts (CEMAGREF), Office National des Forêts (ONF), Services déconcentrés d'appui à la recherche Provence-Alpes-Côte d'Azur (SDAR Paca), Université de Lorraine (UL), Laboratoire Hubert Curien [Saint Etienne] (LHC), Université Jean Monnet [Saint-Étienne] (UJM)-Centre National de la Recherche Scientifique (CNRS)-Institut d'Optique Graduate School (IOGS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Centre National de la Propriété Forestière, and Parc Naturel Régional du Luberon (PNRL)
Subjects: Sylviculture, Ressources génétiques, Diversité génétique, [SDV.EE.ECO]Life Sciences [q-bio]/Ecology, environment/Ecosystems, Potentiel adaptatif, [SDV.BV.BOT]Life Sciences [q-bio]/Vegetal Biology/Botanics, [SDE.BE]Environmental Sciences/Biodiversity and Ecology, [SDV.BID.SPT]Life Sciences [q-bio]/Biodiversity/Systematics, Phylogenetics and taxonomy, Simulation
Abstract: La diversité des capacités d'adaptation est no seulement importante entre essences forestières mais aussi au sein de chaque espèce. La diversité génétique intra-spécifique observée à un instant donné est une "prise de vue" dans une évolution continue. Cette diversité est aussi le carburant nécessaire pour l'évolution des espèces. Pour mieux comprendre les impacts des pratiques de gestion sur la diversité génétique et construire des stratégies d'adaptation à long terme, nous intégrons information génétique et perturbations accidentelles dans des outils existants de simulation d'itinéraires sylvicoles.
Published: 2019

9. A COMBINATION OF GOLD CARBENES AND X-RAYS IS ASSOCIATED WITH CELLULAR AND MITOCHONDRIAL DYSFUNCTIONS IN PROSTATE CANCER CELLS

Author: Eguida, J., Chéron, M., Rivrais, G., Alziari, Serge, Cisnetti, Federico, Gautier, A., Garreau-Balandier, I., Vernet, Patrick, Laboratoire de Physique de Clermont (LPC), Centre National de la Recherche Scientifique (CNRS)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Institut National de Physique Nucléaire et de Physique des Particules du CNRS (IN2P3), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institut National de Physique Nucléaire et de Physique des Particules du CNRS (IN2P3)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Rayet, Béatrice
Subjects: [SDV.CAN] Life Sciences [q-bio]/Cancer, [SDV.CAN]Life Sciences [q-bio]/Cancer
Abstract: International audience; Prostate cancer is the most frequent male cancer and the third cause of death due to a cancer. Cancers are characterized by the perturbation of many cellular parameters such as proliferation, metabolism, in which mitochondria are implied. In this latter is found a very particular DNA population: the mitochondrial DNA (mtDNA). Some mtDNA mutations are correlated to tumorigenesis and cancer progression. These facts strengthen the important role of mitochondria in tumorigenesis
Published: 2018

10. Recent Advances in Transition-Metal-Catalyzed Functionalization of 1-Thiosugars

Author: Samir Messaoudi, Mouad Alami, Nada Ibrahim, Conception, synthèse et vectorisation de biomolécules. (CSVB), Institut Curie-Centre National de la Recherche Scientifique (CNRS)-Université Paris Descartes - Paris 5 (UPD5), Biomolécules : Conception, Isolement, Synthèse (BioCIS), Université Paris-Sud - Paris 11 (UP11)-Université de Cergy Pontoise (UCP), Université Paris-Seine-Université Paris-Seine-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS), Université Paris Descartes - Paris 5 (UPD5)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut Curie [Paris], Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Paris-Sud - Paris 11 (UP11)-Université de Cergy Pontoise (UCP), Université Paris-Seine-Université Paris-Seine, Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Université Paris Descartes - Paris 5 (UPD5)-Institut Curie [Paris]-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Université Paris-Seine-Université Paris-Seine-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: 010405 organic chemistry, Glycomimetic, Chemistry, Organic Chemistry, Electrophile, [CHIM.CATA]Chemical Sciences/Catalysis, 010402 general chemistry, 01 natural sciences, Combinatorial chemistry, 0104 chemical sciences, Thiosugars
Abstract: International audience; Thioglycosides are valuable glycomimetic derivatives that have attracted much attention as mimetics of O-glycosides. Thioglycosides are among the most important glycomimetics reported to date due to their powerful activities. Owing to their importance, building up methods for their construction has drawn considerable attention. However, the classical methods of their synthesis presenting many shortcomings such as the use of harsh acidic media, and are generally limited in substrate scope. Therefore, metal-catalyzed coupling of thiosugars with halogenated electrophiles can be a superior and highly versatile approach to the sunthesis of thioglycosides. The central objective of this Focus Review is to highlight metal-catalyzed reactions for the creation of aromatic and heteroaromatic thioglycosides.
Published: 2018

11. Characterization of a thermotolerant ROK-type mannofructokinase from Streptococcus mitis: application to the synthesis of phosphorylated sugars

Author: Véronique de Berardinis, Ekaterina Darii, Aurélie Fossey-Jouenne, Marcel Salanoubat, Adrien Debard, Jean-Louis Petit, Marielle Lemaire, Stessy Nepert, Virginie Pellouin, Aline Mariage, Christine Guérard-Hélaine, Anne Zaparucha, Carine Vergne-Vaxelaire, Génomique métabolique (UMR 8030), Genoscope - Centre national de séquençage [Evry] (GENOSCOPE), Université Paris-Saclay-Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université Paris-Saclay-Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université d'Évry-Val-d'Essonne (UEVE)-Centre National de la Recherche Scientifique (CNRS), Institut de Chimie de Clermont-Ferrand (ICCF), SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-Université d'Évry-Val-d'Essonne (UEVE), Institut de Chimie de Clermont-Ferrand - Clermont Auvergne (ICCF), Centre National de la Recherche Scientifique (CNRS)-Université Clermont Auvergne (UCA)-Sigma CLERMONT (Sigma CLERMONT), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Centre National de la Recherche Scientifique (CNRS)-Université d'Évry-Val-d'Essonne (UEVE), Association géologique auboise, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA), and Sigma CLERMONT (Sigma CLERMONT)-Université Clermont Auvergne (UCA)-Centre National de la Recherche Scientifique (CNRS)
Subjects: 0301 basic medicine, Thermotolerance, Phosphorylated sugars, Streptococcus mitis, Applied Microbiology and Biotechnology, Fructokinase, Substrate Specificity, Fructokinases, 03 medical and health sciences, chemistry.chemical_compound, Hexokinase, Monosaccharide, [CHIM]Chemical Sciences, Phosphorylation, [SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biochemistry [q-bio.BM], chemistry.chemical_classification, biology, Kinase, Temperature, ROK family, General Medicine, biology.organism_classification, Promiscuity, [SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/Bacteriology, Open reading frame, 030104 developmental biology, Enzyme, chemistry, Biochemistry, Sugars, Biotechnology
Abstract: International audience; Most of the Brepressor, open reading frame, kinase^(ROK) proteins already characterized so far, and exhibiting a kinase activity, take restrictedly D-glucose as substrate. By exploring the sequenced bacterial diversity, 61 ATP-dependent kinases belonging to the ROK family have been identified and experimentally assayed for the phosphorylation of hexoses. These kinases were mainly found to be thermotolerant and highly active toward D-mannose and D-fructose with notable activities toward D-tagatose. Among them, the ATP-dependent kinase from the mesophile Streptococcus mitis (named ScrK mitis) was biochemically characterized and its substrate spectrum further studied. This enzyme possessed impressive catalytic efficiencies toward D-mannose and D-fructose of 1.5 10 6 s −1 M −1 and 2.7 10 5 s −1 M −1 , respectively, but also significant ones toward D-tagatose (3.5 10 2 s −1 M −1) and the unnatural monosaccharides D-altrose (1.1 10 4 s −1 M −1) and D-talose (3.4 10 2 s −1 M −1). Specific activities measured for all hexoses showed a high stereopreference for D-over L-series. As proof of concept, 8 hexoses were phosphorylated in moderate to good yields, some of them described for the first time like L-sorbose-5-phosphate unusually phosphorylated in position 5. Its thermo-tolerance, its wide pH tolerance (from 7 to 10), and temperature range (> 85% activity between 40 and 70°C) open the way to applications in the enzymatic synthesis of monophosphorylated hexoses.
Published: 2018

12. Confirmation of a change in the global shear velocity pattern at around 1000 km depth

Author: Christophe Zaroli, Sophie Lambotte, Eric Debayle, Yanick Ricard, Stéphanie Durand, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Laboratoire de Sciences de la Terre (LST), École normale supérieure - Lyon (ENS Lyon)-Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), Ecole et Observatoire des Sciences de la Terre (EOST), Université de Strasbourg (UNISTRA)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), Institut de physique du globe de Strasbourg (IPGS), Département de sismologie (DS (UMR_7580)), IPG PARIS-Université Paris Diderot - Paris 7 (UPD7)-Centre National de la Recherche Scientifique (CNRS), Institut national des sciences de l'Univers (INSU - CNRS)-Université Louis Pasteur - Strasbourg I-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS), Centre National de la Recherche Scientifique (CNRS)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-École normale supérieure - Lyon (ENS Lyon), Université Paris Diderot - Paris 7 (UPD7)-IPG PARIS-Centre National de la Recherche Scientifique (CNRS), Conseil national de la recherche scientifique du Liban (CNRS Liban), National Council for Scientific Research [Lebanon] (CNRS-L), French National Research Agency (ANR)ANR-11-BLANC-SIMI5-6-016-01European Research Council (ERC)617588Deutsch Forschungsgemeinschaft under the DFG HAADES DU1634/1-1, Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), École normale supérieure de Lyon (ENS de Lyon)-Université Claude Bernard Lyon 1 (UCBL), and Université Paris Diderot - Paris 7 (UPD7)-Institut de Physique du Globe de Paris (IPG Paris)-Centre National de la Recherche Scientifique (CNRS)
Subjects: 010504 meteorology & atmospheric sciences, [SDU.STU.GP]Sciences of the Universe [physics]/Earth Sciences/Geophysics [physics.geo-ph], [SDU.STU]Sciences of the Universe [physics]/Earth Sciences, Geometry, 010502 geochemistry & geophysics, 01 natural sciences, Mantle (geology), Flattening, Physics::Geophysics, Geochemistry and Petrology, Normal mode, Shear velocity, ComputingMilieux_MISCELLANEOUS, 0105 earth and related environmental sciences, Seismic tomography, Surface waves and free oscillations, Spherical harmonics, Geodesy, Wavelength, Body waves, Geophysics, 13. Climate action, Surface wave, Structure of the Earth, Geology
Abstract: In this study, we confirm the existence of a change in the shear velocity spectrum around 1000 km depth based on a new shear velocity tomographic model of the Earth’s mantle, SEISGLOB2. This model is based on Rayleigh surface wave phase velocities, self- and crosscoupling structure coefficients of spheroidal normal modes and body wave traveltimes which are, for the first time, combined in a tomographic inversion. SEISGLOB2 is developed up to spherical harmonic degree 40 and in 21 radial spline functions. The spectrum of SEISGLOB2 is the flattest (i.e. richest in ‘short’ wavelengths corresponding to spherical harmonic degrees greater than 10) around 1000 km depth and this flattening occurs between 670 and 1500 km depth.We also confirmvarious changes in the continuity of slabs and mantle plumes all around 1000 km depth where we also observed the upper boundary of Large Low Shear Velocity Provinces. The existence of a flatter spectrum, richer in short-wavelength heterogeneities, in a region of the mid-mantle can have great impacts on our understanding of the mantle dynamics and should thus be better understood in the future. Although a viscosity increase, a phase change or a compositional change can all concur to induce this change of pattern, its precise origin is still very uncertain.
Published: 2017

13. Expeditious Synthesis of the Topoisomerase I Inhibitors Isoindolo[2,1-b]isoquinolin-7(5H)-one and the Alkaloid Rosettacin Based on Aryl Radical Cyclization of Enamide Generated by Using N-Acyliminium Chemistry

Author: Ata Martin Lawson, Aurélie Namoune, Lahssen El Blidi, Alexandre Bridoux, Sébastien Comesse, Adam Daïch, Vijaykumar D. Nimbarte, Unité de Recherche en Chimie Organique et Macromoléculaire (URCOM), Université Le Havre Normandie (ULH), Normandie Université (NU)-Normandie Université (NU), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Institut de Chimie Pharmaceutique Albert Lespagnol (ICPAL), Université de Lille, Droit et Santé, and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: Aryl radical, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Chemistry, Stereochemistry, Alkaloid, Organic Chemistry, Iminium, [CHIM.CATA]Chemical Sciences/Catalysis, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, Rosettacin, Topoisomerase-I Inhibitor, 010402 general chemistry, Ring (chemistry), 01 natural sciences, Radical cyclization, Catalysis, 0104 chemical sciences, chemistry.chemical_compound, [CHIM.ANAL]Chemical Sciences/Analytical chemistry, [CHIM]Chemical Sciences, ComputingMilieux_MISCELLANEOUS
Abstract: A short and effective approach to the synthesis of the topoisomerase I inhibitor isoindolo[2,1-b]isoquinolin-7(5H)-one and the alkaloid rosettacin belonging to the aromathecin family is presented. The key step of this sequence, which resulted in the formation of a five-membered ring, was the aryl radical cyclization of enamides generated using N-acyliminium chemistry.
Published: 2015

14. Mini-P-gp and P-gp Co-Expression in Brown Trout Erythrocytes: A Prospective Blood Biomarker of Aquatic Pollution

Author: François Desmolles, Bruno Combourieu, Mahchid Bamdad, Christian Amblard, Frédérique Penault-Llorca, Emeline Valton, Laboratoire Microorganismes : Génome et Environnement (LMGE), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Université d'Auvergne - Clermont-Ferrand I (UdA)-Centre National de la Recherche Scientifique (CNRS), Centre National de la Recherche Scientifique (CNRS)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020]), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Centre Jean Perrin [Clermont-Ferrand] (UNICANCER/CJP), UNICANCER, Laboratoire Biochimie Médicale (UMR 384), Institut National de la Santé et de la Recherche Médicale (INSERM), BRICHEUX, Genevieve, Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Clinical Biochemistry, [SDV.MP.PRO] Life Sciences [q-bio]/Microbiology and Parasitology/Protistology, 010501 environmental sciences, [SDV.MP.PRO]Life Sciences [q-bio]/Microbiology and Parasitology/Protistology, 01 natural sciences, Article, Microbiology, 03 medical and health sciences, chemistry.chemical_compound, Brown trout, brown trout, [SDV.EE.SANT] Life Sciences [q-bio]/Ecology, environment/Health, ComputingMilieux_MISCELLANEOUS, 030304 developmental biology, 0105 earth and related environmental sciences, [SDV.EE.SANT]Life Sciences [q-bio]/Ecology, environment/Health, Pollutant, lcsh:R5-920, 0303 health sciences, biology, river pollution, Pesticide, biology.organism_classification, [SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/Bacteriology, In vitro, [SDV.TOX] Life Sciences [q-bio]/Toxicology, Multiple drug resistance, Biomarker, Trout, chemistry, [SDV.TOX]Life Sciences [q-bio]/Toxicology, Environmental chemistry, erythrocytes, mini-P-gp, P-gp, [SDV.MP.BAC] Life Sciences [q-bio]/Microbiology and Parasitology/Bacteriology, blood biomarker, lcsh:Medicine (General), Xenobiotic
Abstract: In aquatic organisms, such as fish, blood is continually exposed to aquatic contaminants. Multidrug Resistance (MDR) proteins are ubiquitous detoxification membrane pumps, which recognize various xenobiotics. Moreover, their expression is induced by a large class of drugs and pollutants. We have highlighted the co-expression of a mini P-gp of 75 kDa and a P-gp of 140 kDa in the primary culture of brown trout erythrocytes and in the erythrocytes of wild brown trout collected from three rivers in the Auvergne region of France. In vitro experiments showed that benzo[a]pyrene, a highly toxic pollutant model, induced the co-expression of mini-P-gp and P-gp in trout erythrocytes in a dose-dependent manner and relay type response. Similarly, in the erythrocytes of wild brown trout collected from rivers contaminated by a mixture of PAH and other multi-residues of pesticides, mini-P-gp and P-gp were able to modulate their expression, according to the nature of the pollutants. The differential and complementary responses of mini-P-gp and P-gp in trout erythrocytes suggest the existence in blood cells of a real protective network against xenobiotics/drugs. This property could be exploited to develop a blood biomarker of river pollution.
Published: 2015

15. Active microorganisms thrive among extremely diverse communities in cloud water

Author: Amato, Pierre, Joly, Muriel, Besaury, Ludovic, Oudart, Anne, Taib, Najwa, Moné, Anne I., Deguillaume, Laurent, Delort, Anne-Marie, Debroas, Didier, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Institut de Chimie de Clermont-Ferrand (ICCF), SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Laboratoire Microorganismes : Génome et Environnement (LMGE), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Université d'Auvergne - Clermont-Ferrand I (UdA)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Météorologie Physique (LaMP), Institut national des sciences de l'Univers (INSU - CNRS)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Université d'Auvergne - Clermont-Ferrand I (UdA)
Subjects: Atmospheric Science, Molecular biology, Atmospheric clouds, [SDV]Life Sciences [q-bio], lcsh:Medicine, Microbiology, Polymerase Chain Reaction, Meteorology, Extraction techniques, Sequencing techniques, Prokaryotic cells, Clouds, [CHIM]Chemical Sciences, Atmospheric Dynamics, Archaean Biology, lcsh:Science, Principal Component Analysis, Bacteria, Atmosphere, Physics, Altitude, lcsh:R, Organisms, Fungi, Biology and Life Sciences, High-Throughput Nucleotide Sequencing, Eukaryota, RNA sequencing, Cell Biology, Atmospheric Physics, RNA extraction, Community structure, Research and analysis methods, Geophysics, Molecular biology techniques, Physical Sciences, [SDE]Environmental Sciences, Earth Sciences, lcsh:Q, France, Cellular Types, Water Microbiology, Research Article
Abstract: International audience; Clouds are key components in Earth’s functioning. In addition of acting as obstacles to light radiations and chemical reactors, they are possible atmospheric oases for airborne microorganisms, providing water, nutrients and paths to the ground. Microbial activity was previously detected in clouds, but the microbial community that is active in situ remains unknown. Here, microbial communities in cloud water collected at puy de Dôme Mountain’s meteorological station (1465 m altitude, France) were fixed upon sampling and examined by high-throughput sequencing from DNA and RNA extracts, so as to identify active species among community members. Communities consisted of ~103−104 bacteria and archaea mL-1 and ~102−103 eukaryote cells mL-1. They appeared extremely rich, with more than 28 000 distinct species detected in bacteria and 2 600 in eukaryotes. Proteobacteria and Bacteroidetes largely dominated in bacteria, while eukaryotes were essentially distributed among Fungi, Stramenopiles and Alveolata. Within these complex communities, the active members of cloud microbiota were identified as Alpha- (Sphingomonadales, Rhodospirillales and Rhizobiales), Beta- (Burkholderiales) and Gamma-Proteobacteria (Pseudomonadales). These groups of bacteria usually classified as epiphytic are probably the best candidates for interfering with abiotic chemical processes in clouds, and the most prone to successful aerial dispersion.
Published: 2017

16. 1,2,4-Triazole-3-thione Compounds as Inhibitors of Dizinc Metallo-β-lactamases

Author: Carine Bebrone, Jean Martinez, Jean-François Hernandez, Lionel Nauton, Laurent Gavara, Gülhan Turan-Zitouni, Filomena De Luca, Paola Sandra Mercuri, Ludovic T. Maillard, Jean Denis Docquier, Silvia Tanfoni, Moreno Galleni, Katja Becker, Pauline Lonjon, Jean-Marie Frère, Laurent Sevaille, Ciarán Condon, Carole Guyon, Maud E. S. Achard, Julia Dzieciolowski, Lionel Benard, Luisa Borgianni, Otto Dideberg, Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Université de Liège, Università degli Studi di Siena = University of Siena (UNISI), Institut de Chimie de Clermont-Ferrand (ICCF), SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Anadolu University, Justus-Liebig-Universität Gießen = Justus Liebig University (JLU), Laboratoire de Biologie Moléculaire et Cellulaire des Eucaryotes (LBMCE), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS), Expression Génétique Microbienne (EGM (UMR_8261 / FRE_3630)), Institut de biologie physico-chimique (IBPC (FR_550)), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Université Paris Diderot - Paris 7 (UPD7)-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Institut National des Sciences Appliquées de Lyon (INSA Lyon), Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-École Supérieure Chimie Physique Électronique de Lyon-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Faculty of Pharmacy Department of Pharmaceutical Chemistry (ANADOLU UNIVERSITY), Justus-Liebig-Universität Gießen (JLU), Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC), Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université Paris Diderot - Paris 7 (UPD7)-Centre National de la Recherche Scientifique (CNRS), Institute of Organic Chemistry, Universität Zürich [Zürich] = University of Zurich (UZH), laboratoire de chimie et pharmacologie de molécules d'intérêt biologique, Service d'Hématologie, Laboratory for Biological Macromolecules [Liège, Belgium], Université de Liège-Center for Protein Engineering-Institut de Chimie B6 [Liège, Belgium], Dipartimento Biotecnol Med, University of Siena, Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM), Anadolu Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, and Institut National des Sciences Appliquées (INSA)-Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS)
Subjects: 0301 basic medicine, Lactams, Stereochemistry, Stenotrophomonas maltophilia, Metalloenzymes, MBL superfamily, 4-Triazole-3-thione, Biochemistry, beta-Lactamases, Nitrogen Heterocycles, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, Antibiotics, Drug Discovery, Hydrolase, 1,2,4-Triazole-3-thione, Bacterial resistance, Metallo-β-Lactamase, β-Lactam antibiotic, Structure–activity relationship, [CHIM]Chemical Sciences, General Pharmacology, Toxicology and Pharmaceutics, Beta-Lactamase Inhibitors, ComputingMilieux_MISCELLANEOUS, Pharmacology, chemistry.chemical_classification, Dose-Response Relationship, Drug, Molecular Structure, biology, Bicyclic molecule, Aryl, Organic Chemistry, Thiones, Active site, Triazoles, bacterial infections and mycoses, biology.organism_classification, Aeromonas hydrophila, 3. Good health, 030104 developmental biology, Enzyme, chemistry, biology.protein, Molecular Medicine, beta-Lactamase Inhibitors, Bacterial Resistance, Bacteria
Abstract: 52nd International Conference on Medicinal Chemistry (RICT) of the French-Medicinal-Chemistry-Society (SCT) - Interfacing Chemical Biology and Drug Discovery -- JUL 06-08, 2016 -- Caen, FRANCE, WOS: 000403905300014, PubMed ID: 28505394, Metallo-beta-lactamases (MBLs) cause resistance of Gram-negative bacteria to beta-lactam antibiotics and are of serious concern, because they can inactivate the last-resort carbapenems and because MBL inhibitors of clinical value are still lacking. We previously identified the original binding mode of 4-amino-2,4-dihydro-5-(2-methylphenyl)-3H-1,2,4-triazole-3-thione (compound IIIA) within the dizinc active site of the L1 MBL. Herein we present the crystallographic structure of a complex of L1 with the corresponding non-amino compound IIIB (1,2-dihydro-5-(2-methylphenyl)-3H-1,2,4-triazole-3-thione). Unexpectedly, the binding mode of IIIB was similar but reverse to that of IIIA. The 3D structures suggested that the triazolethione scaffold was suitable to bind to the catalytic site of dizinc metalloenzymes. On the basis of these results, we synthesized 54 analogues of IIIA or IIIB. Nineteen showed IC50 values in the micromolar range toward at least one of five representative MBLs (i.e., L1, VIM-4, VIM-2, NDM-1, and IMP-1). Five of these exhibited a significant inhibition of at least four enzymes, including NDM-1, VIM2, and IMP-1. Active compounds mainly featured either halogen or bulky bicyclic aryl substituents. Finally, some compounds were also tested on several microbial dinuclear zinc-dependent hydrolases belonging to the MBL-fold superfamily (i.e., endonucleases and glyoxalase II) to explore their activity toward structurally similar but functionally distinct enzymes. Whereas the bacterial tRNases were not inhibited, the best IC50 values toward plasmodial glyoxalase II were in the 10 mm range., French Med Chem Soc, Univ Caen, Agence Nationale de la Recherche ("ANTIMBL") [ANR-14-CE16-0028-01]; Deutsche Forschungsgemeinschaft [BE1540/15-2 within SPP 1710]; Agence Nationale de la Recherche [ANR-06-BLAN-0086], We thank Mr. Pierre Sanchez for mass spectrometry analyses and Wolfram Meyer-Klaucke for advice about tRNase Z. Part of this work was supported by the Agence Nationale de la Recherche ("ANTIMBL", ANR-14-CE16-0028-01, including a fellowship to L.S.), the Deutsche Forschungsgemeinschaft (BE1540/15-2 within SPP 1710 to K.B.), and Agence Nationale de la Recherche ("subtilRNA", ANR-06-BLAN-0086) to C.C.
Published: 2017

17. Palladium-Mediated Labeling of Nucleic Acids

Author: Samir Messaoudi, Eric Defrancq, Département de Chimie Moléculaire - Ingéniérie et Intéractions BioMoléculaires (DCM - I2BM), Département de Chimie Moléculaire (DCM), Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Grenoble Alpes [2016-2019] (UGA [2016-2019])-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Grenoble Alpes [2016-2019] (UGA [2016-2019]), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Bioanalysis, Staining and Labeling, 010405 organic chemistry, Oligonucleotide, Organic Chemistry, Chemical biology, Sonogashira coupling, chemistry.chemical_element, 010402 general chemistry, 01 natural sciences, Biochemistry, Combinatorial chemistry, Catalysis, 0104 chemical sciences, Nucleic Acid Probes, chemistry, Nucleic acid, Molecular Medicine, [CHIM]Chemical Sciences, Molecular Biology, Palladium, ComputingMilieux_MISCELLANEOUS
Abstract: New applications of Pd-catalyzed coupling reactions (Suzuki-Miyaura, Sonogashira, and Stille-Migita coupling) for post-conjugation of nucleic acids have been developed recently. Breakthroughs in this area might now pave the way for the development of sophisticated DNA probes, which might be of great interest in chemical biology, nanotechnology, and bioanalysis, as well as in diagnostic domains.
Published: 2017

18. Well-posedness and optimal decay rates for the viscoelastic Kirchhoff equation

Author: Aissa Guesmia, C Webler, Salim A. Messaoudi, Institut Élie Cartan de Lorraine (IECL), Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Guesmia, Aissa, King Fahd University of Petroleum and Minerals (KFUPM), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: General Mathematics, lcsh:Mathematics, 010102 general mathematics, Mathematical analysis, Well-posedness, Deacay rates, Kirchhoff equation, Kirchhoff integral theorem, lcsh:QA1-939, 01 natural sciences, Viscoelasticity, Domain (mathematical analysis), 010101 applied mathematics, Bounded function, [MATH.MATH-AP]Mathematics [math]/Analysis of PDEs [math.AP], 0101 mathematics, [MATH.MATH-AP] Mathematics [math]/Analysis of PDEs [math.AP], Energy (signal processing), Well posedness, Mathematics
Abstract: International audience; In this paper, we investigate the well-posedness as well as optimal decay rate estimates of the energy associated with a Kirchhoff-Carrier problem in n-dimensional bounded domain under an internal finite memory. The considered class of memory kernels is very wide and allows us to derive new and optimal decay rate estimates then those ones considered previously in the literature for Kirchhoff-type models.
Published: 2017

19. Economic process to produce biohydrogen and volatile fatty acids by a mixed culture using vinasse from sugarcane ethanol industry as nutrient source

Author: Alessandra Cristine Novak, Carlos Ricardo Soccol, Christian Larroche, Régis Nouaille, Luiz Alberto Junior Letti, Vanete Thomaz Soccol, Eduardo Bittencourt Sydney, Satinder Kaur Brar, Saurabh Jyoti Sarma, Institut Pascal (IP), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Centre National de la Recherche Scientifique (CNRS), SIGMA Clermont (SIGMA Clermont)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Laboratoire Microorganismes : Génome et Environnement (LMGE), Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), BRICHEUX, Genevieve, Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Centre National de la Recherche Scientifique (CNRS)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])
Subjects: Environmental Engineering, Vinasse, Microbial Consortia, Industrial Waste, Bioengineering, [SDV.MP.PRO] Life Sciences [q-bio]/Microbiology and Parasitology/Protistology, 7. Clean energy, [SDV.MP.PRO]Life Sciences [q-bio]/Microbiology and Parasitology/Protistology, Industrial waste, Bioreactors, Biogas, Bioenergy, Bioreactor, Biohydrogen, Molasses, Waste Management and Disposal, ComputingMilieux_MISCELLANEOUS, Ethanol, Waste management, Renewable Energy, Sustainability and the Environment, Chemistry, General Medicine, Hydrogen-Ion Concentration, Models, Theoretical, Sugarcane, Fatty Acids, Volatile, Pulp and paper industry, [SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/Bacteriology, Carbon, Saccharum, Biofuel, Biofuels, Volatile fatty acids, Fermentation, [SDV.MP.BAC] Life Sciences [q-bio]/Microbiology and Parasitology/Bacteriology, Biotechnology, Hydrogen
Abstract: This work evaluates the potential of vinasse (a waste obtained at the bottom of sugarcane ethanol distillation columns) as nutrient source for biohydrogen and volatile fatty acids production by means of anaerobic consortia. Two different media were proposed, using sugarcane juice or molasses as carbon source. The consortium LPBAH1 was selected for fermentation of vinasse supplemented with sugarcane juice, resulting in a higher H2 yield of 7.14molH2 molsucrose−1 and hydrogen content in biogas of approx. 31%, while consortium LPBAH2 resulted in 3.66molH2/molsucrose and 32.7% hydrogen content in biogas. The proposed process showed a rational and economical use for vinasse, a mandatory byproduct of the renewable Brazilian energy matrix.
Published: 2014
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20. Multiple paternity in a wild population of Armadillidium vulgare: influence of infection with Wolbachia?

Author: Sophie Beltran-Bech, Frédéric Grandjean, Sylvine Durand, Nicolas Bech, Victorien Valette, Ecologie, Evolution, Symbiose (EES), Ecologie et biologie des interactions (EBI), Université de Poitiers-Centre National de la Recherche Scientifique (CNRS)-Université de Poitiers-Centre National de la Recherche Scientifique (CNRS), Université de Poitiers-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Génétique et biologie des populations de crustacés (GBPC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: 0106 biological sciences, 0301 basic medicine, Male, [SDV]Life Sciences [q-bio], Feminization (biology), Population, Zoology, Paternity, 010603 evolutionary biology, 01 natural sciences, 03 medical and health sciences, Animals, Sex Ratio, Mating, education, ComputingMilieux_MISCELLANEOUS, reproductive and urinary physiology, Ecology, Evolution, Behavior and Systematics, [SDV.EE]Life Sciences [q-bio]/Ecology, environment, Armadillidium vulgare, education.field_of_study, biology, Ecology, Host (biology), biology.organism_classification, Brood, 030104 developmental biology, Wolbachia, Female, Sex ratio, Isopoda, Microsatellite Repeats
Abstract: Female multiple mating has been extensively studied to understand how nonobvious benefits, generally thought to be of genetic nature, could overcome heavy costs such as an increased risk of infection during mating. However, the impact of infection itself on multiple mating has rarely been addressed. The interaction between the bacterium Wolbachia and its terrestrial crustacean host, Armadillidium vulgare, is a relevant model to investigate this question. In this association, Wolbachia is able to turn genetic males into functional females (i.e. feminization), thereby distorting the sex ratio and decreasing the number of available males at the population scale. Moreover, in A. vulgare, females have been shown to mate multiply under laboratory conditions and males prefer uninfected females over infected ones. Additionally, different Wolbachia strains are known to infect A. vulgare and these strains differ in their transmission rate and virulence. All these elements suggest a potential impact of different Wolbachia strains on multiple mating. To investigate this assumption, we collected gravid females in a wild A. vulgare population harbouring both uninfected females and females infected with one of two different Wolbachia strains (wVulM and wVulC) and performed paternity analyses on the obtained broods using microsatellite markers. We demonstrate that (i) multiple paternity is common in this wild population of A. vulgare, with a mean number of fathers of 4.48 ± 1.24 per brood and (ii) females infected with wVulC produced broods with a lower multiple paternity level compared with females infected with wVulM and uninfected ones. This work improves our knowledge of the impact of infections on reproductive strategies.
Published: 2016

21. Structural/textural properties and water reactivity of fluorinated activated carbons

Author: Sébastien Schlienger, Julien Parmentier, Teresa A. Centeno, Elodie Disa, Francis Masin, Marc Dubois, Institut de Science des Matériaux de Mulhouse (IS2M), Université de Haute-Alsace (UHA) Mulhouse - Colmar (Université de Haute-Alsace (UHA))-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Matériaux et Nanosciences Grand-Est (MNGE), Université de Strasbourg (UNISTRA)-Université de Haute-Alsace (UHA) Mulhouse - Colmar (Université de Haute-Alsace (UHA))-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université de Strasbourg (UNISTRA)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS)-Réseau nanophotonique et optique, Université de Strasbourg (UNISTRA)-Université de Haute-Alsace (UHA) Mulhouse - Colmar (Université de Haute-Alsace (UHA))-Centre National de la Recherche Scientifique (CNRS)-Université de Strasbourg (UNISTRA)-Centre National de la Recherche Scientifique (CNRS), MI, Institut de Chimie de Clermont-Ferrand (ICCF), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Matière Condensée et Résonance Magnétique, Université libre de Bruxelles (ULB), Instituto Nacional del Carbon, CSIC-Oviedo, Université de Haute-Alsace (UHA) Mulhouse - Colmar (Université de Haute-Alsace (UHA))-Centre National de la Recherche Scientifique (CNRS), and Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Intercalation (chemistry), Inorganic chemistry, chemistry.chemical_element, 02 engineering and technology, General Chemistry, 010402 general chemistry, 021001 nanoscience & nanotechnology, 01 natural sciences, 0104 chemical sciences, Adsorption, chemistry, Physisorption, 13. Climate action, Desorption, medicine, Fluorine, General Materials Science, Reactivity (chemistry), 0210 nano-technology, Carbon, Activated carbon, medicine.drug
Abstract: International audience; Hydrophobic activated carbons are considered as interesting materials for air or water remediation due to their enhanced affinity for slightly water-soluble organic species. In this context, a commercial activated carbon, in an extruded form, was fluorinated under mild conditions (pure fluorine gas at room temperature) in order to decrease its hydrophilic character and to preserve its microporosity. For comparison, a hydrogenated activated carbon was also prepared by H2 treatment. The resulting samples were characterised by various techniques in order to determine the evolution of the activated carbon materials in terms of composition (XPS, elemental analysis, TGA and NMR) and porosity (nitrogen physisorption (77 K), mercury intrusion and immersion calorimetry). For the fluorinated carbon, the nature of the CFx groups and the strength of the C-F bonds were also investigated using 13C and 19F solid state NMR and TGA techniques. A labile character of the C-F bond, so far exclusively observed for fluorine intercalation compounds, is also shown for the first time for a fluorinated activated carbon by water adsorption/desorption isotherms at room temperature. Care should then be taken for its use in presence of water.
Published: 2012

22. Pharmacological and structural characterization of conformationally restricted (S)-glutamate analogues at ionotropic glutamate receptors

Author: Michael Gajhede, Raminta Venskutonytė, Zeinab Assaf, Darryl S. Pickering, Karla Frydenvang, Lennart Bunch, Lina Juknaitė, David J. Aitken, Sophie Faure, Thierry Gefflaut, Birgitte Nielsen, Jette S. Kastrup, Department of Drug Design and Pharmacology [Copenhagen] (ILF), Faculty of Health and Medical Sciences, University of Copenhagen = Københavns Universitet (KU)-University of Copenhagen = Københavns Universitet (KU), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institut de Chimie Moléculaire et des Matériaux d'Orsay (ICMMO), Université Paris-Sud - Paris 11 (UP11)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), University of Copenhagen = Københavns Universitet (UCPH)-University of Copenhagen = Københavns Universitet (UCPH), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Models, Molecular, Agonist, medicine.drug_class, Stereochemistry, Amino Acid Motifs, Glycine, Kainate receptor, AMPA receptor, Crystallography, X-Ray, 03 medical and health sciences, 0302 clinical medicine, Glutamates, Receptors, Kainic Acid, Structural Biology, medicine, Animals, Receptors, AMPA, Binding site, 030304 developmental biology, 0303 health sciences, Binding Sites, Chemistry, AMPA Kainate Binding affinity Crystal structure Subtype selectivity Structure comparison, Glutamate receptor, Hydrogen Bonding, Stereoisomerism, Ligand (biochemistry), Rats, NMDA receptor, Cyclobutanes, 030217 neurology & neurosurgery, Protein Binding, Ionotropic effect
Abstract: International audience; Conformationally restricted glutamate analogues have been pharmacologically characterized at AMPA and kainate receptors and the crystal structures have been solved of the ligand (2S,10R,20S)-2-(20-carboxycyclobutyl) glycine (CBG-IV) in complex with the ligand binding domains of the AMPA receptor GluA2 and the kainate receptor GluK3. These structures show that CBG-IV interacts with the binding pocket in the same way as (S)-glutamate. The binding affinities reveal that CBG-IV has high affinity at the AMPA and kainate receptor subtypes. Appreciable binding affinity of CBG-IV was not observed at NMDA receptors, where the introduction of the carbocyclic ring is expected to lead to a steric clash with binding site residues. CBG-IV was demonstrated to be an agonist at both GluA2 and the kainate receptor GluK1. CBG-IV showed high affinity binding to GluK1 compared to GluA2, GluK2 and GluK3, which exhibited lower affinity for CBG-IV. The structure of GluA2 LBD and GluK3 LBD in complex with CBG-IV revealed similar binding site interactions to those of (S)-glutamate. No major conformational rearrangements compared to the (S)-glutamate bound conformation were found in GluK3 in order to accommodate CBG-IV, in contrast with GluA2 where a shift in lobe D2 binding site residues occurs, leading to an increased binding cavity volume compared to the (S)-glutamate bound structure.
Published: 2012

23. CuAAC Functionalization of Azide-Tagged Copper(I)-NHCs Acting as Catalyst and Substrate

Author: Daniel Avignant, Clémentine Gibard, Federico Cisnetti, Arnaud Gautier, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), MI, Institut de Chimie de Clermont-Ferrand (ICCF), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Bonnefoy, Stéphanie
Subjects: 010405 organic chemistry, Chemistry, Organic Chemistry, chemistry.chemical_element, Substrate (chemistry), Propargyl alcohol, 010402 general chemistry, 01 natural sciences, Copper, 3. Good health, 0104 chemical sciences, Catalysis, Inorganic Chemistry, chemistry.chemical_compound, Polymer chemistry, Organic chemistry, Surface modification, Azide, Physical and Theoretical Chemistry
Abstract: International audience; Azide-tagged copper(I) complexes of N-heterocyclic carbenes (NHCs) analogous to the well-known bis[2,6- diisopropylphenyl]imidazol-2-ylidene (IPr) and bis[2,6-diisopropylphenyl]imidazolin-2-ylidene (SIPr) were synthesized and characterized. These complexes were able to act as catalyst and substrate in a model copper-catalyzed azide−alkyne (CuAAC) reaction with propargyl alcohol, yielding functionalized copper(I)-NHC complexes.
Published: 2012

24. Synthesis of new C-glycosyl aza-β3-amino acids building blocks

Author: Yves Chapleur, Anne-Sophie Felten, Manuel Andreini, Nadia Pellegrini-Moïse, Hoang-Trang Tran Thien, Claude Taillefumier, Structure et Réactivité des Systèmes Moléculaires Complexes (SRSMC), Institut de Chimie du CNRS (INC)-Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: chemistry.chemical_classification, animal structures, Stereochemistry, Organic Chemistry, macromolecular substances, beta-amino-acid Aza-beta-peptide C-glycosyl compounds Chiral building block, Biochemistry, Reductive amination, Amino acid, carbohydrates (lipids), chemistry.chemical_compound, chemistry, Drug Discovery, [CHIM]Chemical Sciences, Organic chemistry, lipids (amino acids, peptides, and proteins), Glycosyl
Abstract: International audience; New C-glycosylated Nb-protected aza-beta3-amino acid building blocks have been prepared from C-glycosyl aldehydes of gluco and galacto configuration by reductive amination and subsequent N-alkylation. These moieties were elaborated to b-dipeptides by elongation at the C- or the N-terminus establishing their ability to be incorporated in original glycosylated foldamers.
Published: 2012

25. Atmospheric chemistry of carboxylic acids: microbial implication versus photochemistry

Author: Mickaël Vaitilingom, Martine Sancelme, Anne-Marie Delort, Romain Maisonobe, Tiffany Charbouillot, Marius Parazols, Laurent Deguillaume, Pierre Amato, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Photochimie moléculaire et macromoléculaire (PMM), Laboratoire de météorologie physique (LaMP), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC), and Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut national des sciences de l'Univers (INSU - CNRS)
Subjects: [SDU.OCEAN]Sciences of the Universe [physics]/Ocean, Atmosphere, Atmospheric Science, 010504 meteorology & atmospheric sciences, Radical, Inorganic chemistry, 010501 environmental sciences, Biodegradation, Photochemistry, complex mixtures, 01 natural sciences, lcsh:QC1-999, Oxalate, lcsh:Chemistry, Reaction rate, chemistry.chemical_compound, lcsh:QD1-999, chemistry, 13. Climate action, Formate, sense organs, Hydrogen peroxide, Photodegradation, Chemical composition, lcsh:Physics, 0105 earth and related environmental sciences
Abstract: Clouds are multiphasic atmospheric systems in which the dissolved organic compounds, dominated by carboxylic acids, are subject to multiple chemical transformations in the aqueous phase. Among them, solar radiation, by generating hydroxyl radicals (•OH), is considered as the main catalyzer of the reactivity of organic species in clouds. We investigated to which extent the active biomass existing in cloud water represents an alternative route to the chemical reactivity of carboxylic acids. Pure cultures of seventeen bacterial strains (Arthrobacter, Bacillus, Clavibacter, Frigoribacterium, Pseudomonas, Sphingomonas and Rhodococcus), previously isolated from cloud water and representative of the viable community of clouds were first individually incubated in two artificial bulk cloud water solutions at 17 °C and 5 °C. These solutions mimicked the chemical composition of cloud water from "marine" and "continental" air masses, and contained the major carboxylic acids existing in the cloud water (i.e. acetate, formate, succinate and oxalate). The concentrations of these carboxylic compounds were monitored over time and biodegradation rates were determined. In average, they ranged from 2 ×10−19 for succinate to 1 × 10−18 mol cell−1 s−1 for formate at 17 °C and from 4 × 10−20 for succinate to 6 × 10−19 mol cell−1 s−1 for formate at 5 °C, with no significant difference between "marine" and "continental" media. In parallel, irradiation experiments were also conducted in these two artificial media to compare biodegradation and photodegradation of carboxylic compounds. To complete this comparison, the photodegradation rates of carboxylic acids by •OH radicals were calculated from literature data. Inferred estimations suggested a significant participation of microbes to the transformation of carboxylic acids in cloud water, particularly for acetate and succinate (up to 90%). Furthermore, a natural cloud water sample was incubated (including its indigenous microflora); the rates of biodegradation were determined and compared to the photodegradation rates involving •OH radicals. The biodegradation rates in "natural" and "artificial" cloud water were in the same order of magnitude; this confirms the significant role of the active biomass in the aqueous reactivity of clouds.
Published: 2011

26. A 18F-Labeled Fluorobutyl-Substituted Spirocyclic Piperidine Derivative as a Selective Radioligand for PET Imaging of Sigma1 Receptors

Author: Maisonial-Besset, Aurélie, Maisonial, Aurélie, Große Maestrup, Eva, Fischer, Steffen, Hiller, Achim, Scheunemann, Matthias, Wiese, Christian, Schepmann, Dirk, Steinbach, Jörg, Deuther-Conrad, Winnie, Wünsch, Bernhard, Brust, Peter, Imagerie Moléculaire et Stratégies Théranostiques (IMoST), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020]), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institute of Radiopharmacy, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Westfälische Wilhelms-Universität Münster (WWU), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Westfälische Wilhelms-Universität Münster = University of Münster (WWU)
Subjects: Biodistribution, Stereochemistry, Biochemistry, 03 medical and health sciences, 0302 clinical medicine, In vivo, Drug Discovery, Side chain, Haloperidol, medicine, Radioligand, [CHIM]Chemical Sciences, General Pharmacology, Toxicology and Pharmaceutics, Receptor, ComputingMilieux_MISCELLANEOUS, 030304 developmental biology, Pharmacology, 0303 health sciences, [CHIM.ORGA]Chemical Sciences/Organic chemistry, Chemistry, Organic Chemistry, Radiosynthesis, 030220 oncology & carcinogenesis, Molecular Medicine, Specific activity, [CHIM.RADIO]Chemical Sciences/Radiochemistry, medicine.drug
Abstract: In this study, we synthesized and evaluated a new spirocyclic piperidine derivative 3, containing a 4-fluorobutyl side chain, as a PET radioligand for neuroimaging of σ₁ receptors. In vitro, compound 3 displayed high affinity for σ₁ receptors (K(i) =1.2 nM) as well as high selectivity. [¹⁸F]3 radiosynthesis was performed from the corresponding tosylate precursor, with high radiochemical yield (45-51 %), purity (>98 %), and specific activity (>201 GBq μmol⁻¹). Metabolic stability of [¹⁸F]3 in the brain of CD-1 mice was verified, and no penetration of peripheral radiometabolites into the cerebral tissue was observed. Results of ex vivo autoradiography revealed that the distribution of [¹⁸F]3 in the brain corresponded to regions with high σ₁ receptor density. The highest region-specific total-to-nonspecific ratio was determined in the facial nucleus (4.00). Biodistribution studies indicated rapid and high levels in brain uptake of [¹⁸F]3 (2.2 % ID per gram at 5 min p.i.). Pre-administration of haloperidol significantly inhibited [¹⁸F]3 uptake into the brain and σ₁ receptor-expressing organs, further confirming in vivo target specificity.
Published: 2011

27. Effect of Fluorination and Size of the Alkyl Side-Chain on the Solubility of Carbon Dioxide in 1-Alkyl-3-methylimidazolium Bis(trifluoromethylsulfonyl)amide Ionic Liquids

Author: Jean Yves Coxam, D. Almantariotis, Agilio A. H. Padua, M. F. Costa Gomes, Thierry Gefflaut, Thermodynamique et Interactions Moléculaires (LTIM), Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), ADEME, IDRIS, and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: chemistry.chemical_classification, Inorganic chemistry, Solvation, 02 engineering and technology, 010402 general chemistry, 021001 nanoscience & nanotechnology, 01 natural sciences, 0104 chemical sciences, Surfaces, Coatings and Films, [CHIM.THEO]Chemical Sciences/Theoretical and/or physical chemistry, chemistry.chemical_compound, chemistry, Amide, Carbon dioxide, Ionic liquid, Materials Chemistry, Physical chemistry, Physical and Theoretical Chemistry, Alkyl side chain, Solubility, 0210 nano-technology, ComputingMilieux_MISCELLANEOUS, Alkyl, Bar (unit)
Abstract: It is proven in this work that it is possible to significantly increase the carbon dioxide uptake by an ionic liquid relying on physical interactions only. The solubility and thermodynamics of solvation of carbon dioxide in the ionic liquids 1-octyl-3-methylimidazolium bis[trifluoromethylsulfonyl]amide [C(8)mim][Ntf(2)], 1-decyl-3-methylimidazolium bis[trifluoromethylsulfonyl]amide [C(10)mim][Ntf(2)], and 1-(3,3,4,4,5,5,6,6,7,7,8,8,8-tridecafluorooctyl)-3-methylimidazolium bis[trifluoromethylsulfonyl]amide [C(8)H(4)F(13)mim][Ntf(2)] were determined experimentally between 298 and 343 K at pressures close to atmospheric. The solubility of carbon dioxide is significantly higher in the fluorine-substituted ionic liquid with Henry's law constants at 303 K of 33.3 and 30.7 bar for [C(8)mim][Ntf(2)] and [C(10)mim][Ntf(2)], respectively, and of 28.0 bar for [C(8)H(4)F(13)mim][Ntf(2)]. Molecular simulation was used for interpreting the molecular mechanisms of solvation of carbon dioxide in the studied ionic liquids and coherent molecular mechanisms of solvation are proposed in light of the solute-solvent radial distribution functions. It is shown that the increase of the size of the hydrogenated or fluorinated alkyl chain in the imidazolium cation does not lead to a steady augmentation of the gaseous uptake by the liquid probably due to an increase of the nonpolar domains of the ionic liquid, carbon dioxide being solvated preferentially in the charged regions of the solvent.
Published: 2010

28. Synthesis, kinase inhibitory potencies and in vitro antiproliferative activity of isoindigo and 7′-azaisoindigo derivatives substituted by Sonogashira cross-coupling

Author: Pascale Moreau, Fadoua Bouchikhi, Fabrice Anizon, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Indoles, Stereochemistry, Isoindigos, Sonogashira coupling, Antineoplastic Agents, HL-60 Cells, Stereoisomerism, Protein Serine-Threonine Kinases, 010402 general chemistry, 01 natural sciences, Chemical synthesis, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, Humans, Structure–activity relationship, Protein Kinase Inhibitors, Antitumour agents, Cell Proliferation, Pharmacology, Molecular Structure, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Chemistry, Kinase, Organic Chemistry, General Medicine, Indigoids, In vitro, 0104 chemical sciences, Kinase inhibitors, Lactam, Casein kinase 1, Drug Screening Assays, Antitumor, K562 Cells
Abstract: International audience; In the course of structure–activity relationship studies we were interested in the synthesis of isoindigo and 7′-azaisoindigo derivatives substituted at the N-1 position by a 1-(2,3,4,6-tetra-O-acetyl-β-d-glucopyranosyl), at the 5′-position by various chains introduced by Sonogashira cross-coupling and substituted or not at the 5-position by a bromine atom. To get an insight into the substitution pattern required for the best biological potencies, their kinase inhibitory potencies and their in vitro antiproliferative activities were evaluated. The derivatives were tested toward four protein kinases (CDK5/p25, GSK3, CK1, Dyrk1A) and their in vitro antiproliferative activity was tested against two human myeloid leukaemia cell lines (K562 and HL60).
Published: 2009

29. Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors — Focus on subtypes iGlu5–7

Author: Sébastien Alaux, Lennart Bunch, Thierry Gefflaut, Darryl S. Pickering, Emmanuelle Sagot, Brigitte Nielsen, Department of Medicinal Chemistry, University of Copenhagen = Københavns Universitet (KU), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Department of Pharmacology and Pharmacotherapy [Copenhagen], Faculty of Pharmaceutical Sciences [Copenhagen] (FARMA), University of Copenhagen = Københavns Universitet (KU)-University of Copenhagen = Københavns Universitet (KU), University of Copenhagen = Københavns Universitet (UCPH), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and University of Copenhagen = Københavns Universitet (UCPH)-University of Copenhagen = Københavns Universitet (UCPH)
Subjects: Models, Molecular, Kainic acid, Subtype selectivity, Stereochemistry, Molecular Conformation, Glutamic Acid, Kainate receptor, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, AMPA receptor, Biology, Ligands, Sensitivity and Specificity, 01 natural sciences, Inhibitory Concentration 50, Radioligand Assay, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, Animals, Receptor, Neurotransmitter, 030304 developmental biology, Pharmacology, 0303 health sciences, Kainic Acid, Molecular Structure, 010405 organic chemistry, Glutamate receptor, Rats, 3. Good health, 0104 chemical sciences, iGlu7, Kinetics, iGlu6, iGlu5, Receptors, Glutamate, Biochemistry, chemistry, NMDA receptor, Propionates, Ionotropic effect
Abstract: International audience; The kainic acid (kainate, KA) receptors belong to the class of ionotropic glutamate (iGlu) receptors in the central nervous system. Five subtypes have been identified, which have been termed KA1,2 and iGlu5–7. In the search for subtype selective ligands, α-amino-5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA), (4R)-methyl Glu (1a), and E-4-neopentylidene Glu (2f) have all previously been reported as selective agonists for the iGlu5 receptor subtype. In this paper, we present the pharmacological evaluation of a five-compound series of (4R)-alkyl Glu analogs (1b–e,g) which may be envisaged as conformationally released designs of ATPA and 4-alkylidenes 2a–h. Most notable is the pharmacological profile for (4R)-isopentyl Glu (1g) which shows a 10-fold increase in binding affinity for the iGlu5 receptor subtype (Ki = 20.5 nM) in comparison with its E-4-alkylidene structural isomer 2g. Furthermore, 1g displays high selectivity over other KA receptor subtypes (KA1,2 and iGlu6,7), AMPA-, and NMDA receptors (2050 and > 5000 fold, respectively)
Published: 2009

30. Pumice stone supported titanium dioxide for removal of pathogen in drinking water and recalcitrant in wastewater

Author: Machiraju Subrahmanyam, D. Naveen Kumar, Pierre Boule, Martine Sancelme, V. Durga Kumari, Anita Rachel, Photochimie moléculaire et macromoléculaire (PMM), Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Pellets, 02 engineering and technology, 010501 environmental sciences, 01 natural sciences, law.invention, chemistry.chemical_compound, law, Pumice, TiO2, General Materials Science, Photocatalysis, Filtration, 0105 earth and related environmental sciences, Cement, Renewable Energy, Sustainability and the Environment, Chemistry, technology, industry, and agriculture, 021001 nanoscience & nanotechnology, 6. Clean water, Disinfection, Pumice stone, Wastewater, Chemical engineering, Titanium dioxide, Water treatment, Detoxification, 0210 nano-technology
Abstract: International audience; Bactericidal and organic degradation effects of TiO2 on pumice stone are described in this paper. Immobilization of TiO2 on pumice stone is easy and efficient method to obtain photocatalytic reactions without the problem of filtration. Pumice stone is soft and available as pellets that can be used in pellets fixed (with cement or poly carbonate) on a slanting plank/glass by coating the preformed TiO2 over the pellets using simple paint brush for applying the photo catalyst. The treatment of inactivation of bacteria especially E. coli existing in real river waters and also different model organic substrate degradations like acid orange-7, resorcinol, 4, 6-dinitro-o-cresol, 4-nitrotoluene-2-sulfonicacid, isoproturan are studied. Furthermore, TiO2 over pumice stone loaded in a multi tube reactor gave similar results for the disinfection and detoxification studies
Published: 2008

31. Microbiology and atmospheric processes: chemical interactions of primary biological aerosols

Author: Maud Leriche, Ulrich Pöschl, Parisa A. Ariya, Nadine Chaumerliac, Anne-Marie Delort, Cindy E. Morris, H. Bauer, Andrea I. Flossmann, Pierre Amato, Laurent Deguillaume, Laboratoire de météorologie physique (LaMP), Centre National de la Recherche Scientifique (CNRS)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP), Laboratoire d'aérologie (LA), Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Observatoire Midi-Pyrénées (OMP), Institut de Recherche pour le Développement (IRD)-Centre National de la Recherche Scientifique (CNRS)-Université Fédérale Toulouse Midi-Pyrénées-Centre National d'Études Spatiales [Toulouse] (CNES)-Météo France-Institut de Recherche pour le Développement (IRD)-Centre National de la Recherche Scientifique (CNRS)-Centre National d'Études Spatiales [Toulouse] (CNES)-Météo France-Centre National de la Recherche Scientifique (CNRS), SEESIB, Centre National de la Recherche Scientifique (CNRS)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut national des sciences de l'Univers (INSU - CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS), Department of Atmospheric and Oceanic Sciences [Montréal], McGill University = Université McGill [Montréal, Canada], Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS), Max Planck Institute for Chemistry (MPIC), Max-Planck-Gesellschaft, Inst. for Chemical Technologies and Analytics, Vienna University of Technologies, Unité de Pathologie Végétale, Institut National de la Recherche Agronomique (INRA), Laboratoire de Météorologie Physique (LaMP), Institut national des sciences de l'Univers (INSU - CNRS)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Laboratoire d'aérologie (LAERO), Université de Toulouse (UT)-Université de Toulouse (UT)-Observatoire Midi-Pyrénées (OMP), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National d'Études Spatiales [Toulouse] (CNES)-Centre National de la Recherche Scientifique (CNRS)-Météo-France -Institut de Recherche pour le Développement (IRD)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National d'Études Spatiales [Toulouse] (CNES)-Centre National de la Recherche Scientifique (CNRS)-Météo-France -Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Biogeochemistry Department, Max-Planck-Institut für Plasmaphysik [Garching] (IPP), Vienna University of Technology, Unité de Pathologie Végétale (PV), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS)-Synthèse et étude de systèmes à intêret biologique (SEESIB), Centre National de la Recherche Scientifique (CNRS)-Observatoire Midi-Pyrénées (OMP), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées, McGill University, Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), Météo France-Centre National d'Études Spatiales [Toulouse] (CNES)-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Météo France-Centre National d'Études Spatiales [Toulouse] (CNES)-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: ATMOSPHERIC PROCESS, AEROSOL, FUNGI, BACTERIA, AIRBORNE MICROORGANISM, PROCESSUS ATMOSPHERIQUE, DISSEMINATION MICROBIOLOGIQUE, 010504 meteorology & atmospheric sciences, Biodiversité et Ecologie, [SDE.MCG]Environmental Sciences/Global Changes, lcsh:Life, Chemical interaction, champignon pathogène, 010501 environmental sciences, 01 natural sciences, Atmosphere, Biodiversity and Ecology, Nutrient, [CHIM.ANAL]Chemical Sciences/Analytical chemistry, lcsh:QH540-549.5, température, microbiologie, Milieux et Changements globaux, Ecology, Evolution, Behavior and Systematics, Earth-Surface Processes, 0105 earth and related environmental sciences, bactérie, Primary (chemistry), climat, Chemistry, lcsh:QE1-996.5, Particulates, Snow, environnement, Aerosol, lcsh:Geology, lcsh:QH501-531, 13. Climate action, Atmospheric chemistry, Environmental chemistry, lcsh:Ecology, [SDE.BE]Environmental Sciences/Biodiversity and Ecology
Abstract: This paper discusses the influence of primary biological aerosols (PBA) on atmospheric chemistry and vice versa through microbiological and chemical properties and processes. Several studies have shown that PBA represent a significant fraction of air particulate matter and hence affect the microstructure and water uptake of aerosol particles. Moreover, airborne micro-organisms, namely fungal spores and bacteria, can transform chemical constituents of the atmosphere by metabolic activity. Recent studies have emphasized the viability of bacteria and metabolic degradation of organic substances in cloud water. On the other hand, the viability and metabolic activity of airborne micro-organisms depend strongly on physical and chemical atmospheric parameters such as temperature, pressure, radiation, pH value and nutrient concentrations. In spite of recent advances, however, our knowledge of the microbiological and chemical interactions of PBA in the atmosphere is rather limited. Further targeted investigations combining laboratory experiments, field measurements, and modelling studies will be required to characterize the chemical feedbacks, microbiological activities at the air/snow/water interface supplied to the atmosphere.
Published: 2008

32. Cyclic β-Peptoids

Author: Claude Taillefumier, Sophie Faure, Claude Didierjean, Vincent Théry, Olivier Roy, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Cristallographie, Résonance Magnétique et Modélisations (CRM2), Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: [CHIM.ORGA]Chemical Sciences/Organic chemistry, Stereochemistry, Organic Chemistry, Stereoisomerism, Crystal structure, Ring (chemistry), Biochemistry, Combinatorial chemistry, chemistry.chemical_compound, Protein structure, Template, chemistry, Tetramer, Physical and Theoretical Chemistry, Quantum, Derivative (chemistry)
Abstract: The first synthesis of functionalized beta-peptoid macrocycles is reported. X-ray crystallographic structure of tetramer 9 reveals a C2-symmetrical derivative with unexpected all-cis-amide bonds and spatial disposition of the appendages toward the two opposite faces of the ring. Quantum calculations suggest that 9 is locked in this layout. These macrocycles constitute novel promising templates for multimeric ligation of biologically active ligands. The concept was exemplified by chemical decoration of tetramer 9 via "click" reactions.
Published: 2008

33. Biotransformation of nitriles to amides using soluble and immobilized nitrile hydratase from Rhodococcus erythropolis A4

Author: Marek Kuzma, Marielle Lemaire, Ludmila Martínková, Vladimír Křen, Jean Bolte, Miroslav Pátek, Estelle Gallienne, Kristýna Slámová, Lutz Fischer, Sabine Lutz-Wahl, Andrea Tóthová, Sander van Pelt, Vojtěch Vejvoda, Ondřej Kaplan, Helena Pelantová, Veronika Elišáková, David Kubáč, Institute of biotechnology, Czech Academy of Sciences [Prague] (CAS), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institute of Food Science and Biotechnlogy, University of Hohenheim, Laboratory of Biocatalysis and Organic Chemistry, Delft University of Technology (TU Delft), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Immobilized enzyme, Nitrile, Bioengineering, Nitrile hydratase, 01 natural sciences, Biochemistry, Catalysis, Amidase, 03 medical and health sciences, chemistry.chemical_compound, Biotransformation, Branched and substituted nitriles, Cross-linked enzyme aggregates, Amidase activity, Organic chemistry, Rhodococcus erythropolis, 030304 developmental biology, chemistry.chemical_classification, 0303 health sciences, biology, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Chemistry, Process Chemistry and Technology, biology.organism_classification, 0104 chemical sciences, Enzyme, Bacteria
Abstract: A semi-purified nitrile hydratase from Rhodococcus erythropolis A4 was applied to biotransformations of 3-oxonitriles 1a–4a, 3-hydroxy-2-methylenenitriles 5a–7a, 4-hydroxy-2-methylenenitriles 8a–9a, 3-hydroxynitriles 10a–12a and 3-acyloxynitrile 13a into amides 1b–13b. Cross-linked enzyme aggregates (CLEAs) with nitrile hydratase and amidase activities (88% and 77% of the initial activities, respectively) were prepared from cell-free extract of this microorganism and used for nitrile hydration in presence of ammonium sulfate, which selectively inhibited amidase activity. The genes nha1 and nha2 coding for α and β subunits of nitrile hydratase were cloned and sequenced.
Published: 2008

34. Synthesis and Biological Activities of New Checkpoint Kinase 1 Inhibitors Structurally Related to Granulatimide

Author: Elisabeth Conchon, Michelle Prudhomme, Fabrice Anizon, Bettina Aboab, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Models, Molecular, Molecular model, Stereochemistry, Carbazoles, Antineoplastic Agents, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, 010402 general chemistry, 01 natural sciences, Chemical synthesis, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Alkaloids, Cell Line, Tumor, Drug Discovery, Animals, Humans, Moiety, Imidazole, Structure–activity relationship, CHEK1, Protein Kinase Inhibitors, Indole test, 010405 organic chemistry, 3. Good health, 0104 chemical sciences, Quinone, chemistry, Checkpoint Kinase 1, Molecular Medicine, Drug Screening Assays, Antitumor, biological phenomena, cell phenomena, and immunity, Protein Kinases
Abstract: In the course of structure-activity relationship studies on granulatimide analogues, new pyrrolo[3,4-c]carbazoles in which the imidazole heterocycle has been replaced by a five- or a six-membered ring bearing one or two carbonyl functions have been synthesized. Their checkpoint kinase 1 (Chk1) inhibitory properties and their in vitro antiproliferative activities toward three tumor cell lines-murine leukemia L1210 and human colon carcinoma HT29 and HCT116 have been determined. The results of molecular modeling in the ATP binding pocket of Chk1 are described. Among the newly synthesized compounds, compounds 13 and 16, in which the imidazole was replaced by a quinone and a hydroquinone and which bear a hydroxy group on the indole moiety, are the most potent Chk1 inhibitors in this series with IC50 values of 27 and 23 nM, respectively.
Published: 2007

35. Chemoenzymatic Synthesis of Glutamic Acid Analogues: Substrate Specificity and Synthetic Applications of Branched Chain Aminotransferase from Escherichia coli

Author: Emmanuelle Sagot, Thierry Gefflaut, Sébastien Alaux, Mo Xian, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: chemistry.chemical_classification, Ozonolysis, 010405 organic chemistry, Chemistry, Stereochemistry, Branched chain aminotransferase, Organic Chemistry, Glutamic Acid, Substrate (chemistry), Glutamic acid, 010402 general chemistry, medicine.disease_cause, 01 natural sciences, Chemical synthesis, Enol, Substrate Specificity, 0104 chemical sciences, Kinetics, chemistry.chemical_compound, Enzyme, Escherichia coli, medicine, Ketoglutaric Acids, Transaminases
Abstract: A new route to alpha-keto acids is described, based on the ozonolysis of enol acetates obtained from alpha-substituted beta-keto esters. Escherichia coli branched chain aminotransferase (BCAT) activity toward a variety of substituted 2-oxoglutaric acids was demonstrated analytically. BCAT was shown to have a broad substrate spectrum, complementary to that of aspartate aminotransferase, and to offer access to a variety of glutamic acid analogues. The usefulness of BCAT was demonstrated through the synthesis of several 3- and 4-substituted derivatives.
Published: 2007

36. Genome Mining for Innovative Biocatalysts: New Dihydroxyacetone Aldolases for the Chemist’s Toolbox

Author: Alain Perret, Marielle Besnard-Gonnet, Véronique de Berardinis, Marine Debacker, Virginie Pellouin, Jean-Louis Petit, Marcel Salanoubat, Adrien Debard, Marielle Lemaire, Aline Mariage, Virgil Hélaine, Ekaterina Darii, Carlos A. F. Fernandes, Martine Sancelme, Christine Guérard-Hélaine, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Génomique métabolique (UMR 8030), Genoscope - Centre national de séquençage [Evry] (GENOSCOPE), Université Paris-Saclay-Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université Paris-Saclay-Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université d'Évry-Val-d'Essonne (UEVE)-Centre National de la Recherche Scientifique (CNRS), Institut de Chimie de Clermont-Ferrand (ICCF), SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Sigma CLERMONT (Sigma CLERMONT), SIGMA Clermont (SIGMA Clermont)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP), Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-Université d'Évry-Val-d'Essonne (UEVE), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Centre National de la Recherche Scientifique (CNRS)
Subjects: [SDV.BIO]Life Sciences [q-bio]/Biotechnology, biocatalysis, [SDV]Life Sciences [q-bio], enzymes, Dihydroxyacetone, 01 natural sciences, Catalysis, Inorganic Chemistry, 03 medical and health sciences, chemistry.chemical_compound, Aldol reaction, Sequence comparison, biocatalysis, C[BOND]C coupling, enzymes, gene expression, mass spectrometry, [CHIM]Chemical Sciences, [SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology, Physical and Theoretical Chemistry, 030304 developmental biology, mass spectrometry, chemistry.chemical_classification, 0303 health sciences, Multiple sequence alignment, biology, 010405 organic chemistry, Organic Chemistry, Aldolase A, [CHIM.CATA]Chemical Sciences/Catalysis, 0104 chemical sciences, Enzyme, chemistry, Biochemistry, Biocatalysis, biology.protein, C[BOND]C coupling, gene expression, Genome mining
Abstract: International audience; Stereoselective carboligating enzymes were discovered by a genome mining approach to extend the biocatalysis toolbox. Seven hundred enzymes were selected by sequence comparison from diverse prokaryotic species as representatives of the aldolase (FSA) family diversity. The aldol reaction tested involved dihydroxyacetone (DHA) and glyceraldehyde-3-phosphate. The hexose-6-phosphate formation was monitored by mass spectrometry. Eighteen enzymes annotated either as transaldolases or aldolases were found to exhibit a DHA aldolase activity. Remarkably, six of them proven as aldolases, and not transaldolases, shared very limited similarities with those currently described. Multiple sequence alignment performed on all enzymes revealed a Tyr in the new DHA aldolases as found in FSAcoli instead of a Phe usually found in transaldolases. Four of these DHA aldolases were biochemically characterised in comparison with FSAcoli. In particular, an aldolase from Listeria monocytogenes exhibited interesting catalytic properties.
Published: 2015

37. Synthesis and antiproliferative activities of indolin-2-one derivatives bearing amino acid moieties

Author: Mathieu Sassatelli, Michelle Prudhomme, Eric Debiton, Pascale Moreau, Bettina Aboab, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Primary culture, Indoles, Magnetic Resonance Spectroscopy, Spectrophotometry, Infrared, Stereochemistry, 030303 biophysics, Antineoplastic Agents, Indolin 2 one, 010402 general chemistry, Murine fibroblast, 01 natural sciences, Chemical synthesis, Mass Spectrometry, 03 medical and health sciences, chemistry.chemical_compound, Drug Discovery, medicine, Solid tumor, Fibroblast, Cytotoxicity, 030304 developmental biology, Pharmacology, chemistry.chemical_classification, 0303 health sciences, Bicyclic molecule, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Organic Chemistry, Antiproliferative activities, General Medicine, In vitro, Indolin-2-ones, 3. Good health, 0104 chemical sciences, Amino acid, medicine.anatomical_structure, Biochemistry, chemistry, Cell culture, Lactam, Amino acids
Abstract: A convenient synthesis of indolin-2-ones substituted in the 3 position by an aminomethylene group bearing different amino acid moieties is described. Their antiproliferative activities were evaluated toward a panel of human solid tumor cell lines (PC 3, DLD-1, MCF-7, M4 Beu, A549, PA 1) and healthy cell lines (a murine fibroblast L929 and a human fibroblast primary culture).
Published: 2006

38. Synthesis of stereochemical probes for new fluorogenic assays for yeast transketolase variants

Author: Angelika Lásiková, Virgil Hélaine, Aurélie Sevestre, Laurence Hecquet, Franck Charmantray, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Chemistry, Stereochemistry, High-throughput screening, Organic Chemistry, Mutant, Wild type, Mutagenesis (molecular biology technique), Tartrate, Transketolase, 010402 general chemistry, C-C bond formation, 01 natural sciences, Biochemistry, Yeast, Enzyme evolution, 0104 chemical sciences, chemistry.chemical_compound, High throughput screening, Drug Discovery, Stereoselectivity, Fluorogenic assays
Abstract: For the screening of yeast transketolase (TK) variants with improved or new properties acquired by random mutagenesis, we report on the stereoselective synthesis of fluorogenic substrates as probes for measuring TK activity. Compound 1 (7-(2′,3′,5′-trihydroxy-4′-oxo-pentyl)oxycoumarine), prepared as previously described, [Tetrahedron Lett. 2003, 44, 827–830] enabled us to evaluate wild type TK velocity in a simple, specific and reproducible way. To select TK mutants able to produce d-threo aldoses, we prepared compound 2 (dihydroxy-4-O-(2′-oxo-benzopyran-7′-yl-D-threose) from dimethyl tartrate. Starting from d-ribose, we successfully obtained compound 3 (7′-(2,3,5-trihydroxy-4-oxo-pentyl)oxycoumarine) as a probe for TK mutants able to produce l-erythro ketoses.
Published: 2006

39. Synthesis of pyridino[3′,2′:4,5]pyrrolo[3,2-g]pyrrolo[3,4-e]indolizin-1,3-dione and pyrrolo[3,2-c]pyrazole skeletons

Author: Bruno Pfeiffer, Michelle Prudhomme, Fabrice Anizon, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Indole test, Isogranulatimide, Antitumor agents, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Stereochemistry, 7-Azaindole, Organic Chemistry, Pyrazole, 010402 general chemistry, 2-c]pyrazole, 01 natural sciences, Biochemistry, G2 Checkpoint inhibitors, 0104 chemical sciences, chemistry.chemical_compound, chemistry, Drug Discovery, Imidazole, Moiety, Pyrrolo[3, Pyrrole
Abstract: A three step synthesis of an isogranulatimide analogue, in which the imidazole moiety is replaced by a pyrrole unit and the indole heterocycle is replaced by a 7-azaindole moiety is described. Moreover, a novel synthetic pathway to the pyrrolo[3,2- c ]pyrazole skeleton is reported.
Published: 2006

40. Biotransformation of the triketone herbicide mesotrione by aBacillus strain. Metabolite profiling using liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectrometry

Author: Bertrand Legeret, Pascale Besse-Hoggan, Martine Sancelme, Anne-Marie Delort, Bruno Combourieu, Stéphanie Durand, Anne-Sophie Martin, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Spectrometry, Mass, Electrospray Ionization, Metabolite, Electrospray ionization, Bacillus, 010501 environmental sciences, Mass spectrometry, 01 natural sciences, Analytical Chemistry, Mesotrione, chemistry.chemical_compound, Hydroxylamine, Biotransformation, [CHIM.ANAL]Chemical Sciences/Analytical chemistry, Liquid chromatography–mass spectrometry, Chromatography, High Pressure Liquid, Spectroscopy, 0105 earth and related environmental sciences, Chromatography, Cyclohexanones, Herbicides, 010401 analytical chemistry, Organic Chemistry, 0104 chemical sciences, Metabolic pathway, chemistry
Abstract: The metabolic pathway involved in the biotransformation of the herbicide mesotrione by the bacterial strain Bacillus sp. 3B6 was investigated by a reliable liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectrometry (LC/ESI-QTOF-MS) method. The LC/ESI-MS method, both in positive and negative mode, with the assistance of MS(2) fragments and isotopic pattern analyses, allowed us to identify five metabolites. This work constitutes the first complete monitoring of mesotrione degradation kinetics. Among the transformation products found by both techniques, one was formed by intramolecular cyclization between a hydroxylamine and a keto function, which is quite a rare biological reactivity process. For each identified metabolite, a fragmentation pathway is proposed for negative and positive mode.
Published: 2006

41. Macro- and Nanotribological Properties of Graphite Tribofilms: Influence of the Sliding Interface

Author: P. Thomas, Nadiège Nomède-Martyr, Laurence Romana, Georges Minatchy, Philippe Bilas, Agence Universitaire de la Francophonie (AUF), Groupe de Technologie des Surfaces et Interfaces (GTSI), Université des Antilles (UA), MI, Institut de Chimie de Clermont-Ferrand (ICCF), Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-SIGMA Clermont (SIGMA Clermont)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Sigma CLERMONT (Sigma CLERMONT)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Sigma CLERMONT (Sigma CLERMONT)-Centre National de la Recherche Scientifique (CNRS), Groupe de Technologie des Surfaces et Interfaces [URp2_2] (GTSI), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Materials science, Nanostructure, Silicon, Alloy, chemistry.chemical_element, Nanotechnology, engineering.material, [SPI]Engineering Sciences [physics], chemistry.chemical_compound, Shear strength, [CHIM]Chemical Sciences, Graphite, Composite material, [PHYS.COND]Physics [physics]/Condensed Matter [cond-mat], ComputingMilieux_MISCELLANEOUS, [PHYS]Physics [physics], Mechanical Engineering, technology, industry, and agriculture, Surfaces and Interfaces, Surfaces, Coatings and Films, chemistry, Silicon nitride, Mechanics of Materials, Nanotribology, engineering, Carbon
Abstract: Macrotribological studies of microcrystalline graphite powder reveal a drastic decrease in the friction coefficient when the experiments are carried out in the presence of low-viscosity liquids. The friction reduction is attributed to the simultaneous presence of particles and liquid in the sliding contact, but the mechanisms involved remain unclear. In order to contribute to the understanding of liquid action in friction reduction mechanisms, nanoscale investigations of the tribofilms have been performed using lateral force microscopy. Attention is devoted to the nanostructure of the film surfaces and their nanofriction behavior using an atomic force microscope. The influence of the tip/sample interfaces on friction properties is investigated by using AFM tips constituted of different compounds (silicon, gold/chromium alloy, silicon nitride or carbon-covered AFM tip) and by performing the nanofriction tests in air or liquid environments. The results indicate that the friction reduction observed at macroscale is attributed neither to the lowering of the shear strength of the carbon/carbon interface in the presence of liquid nor to the nanostructure of the film surface. Collective liquid/particles effects inside the contact during sliding are probably involved.
Published: 2014

42. 1 H Nuclear Magnetic Resonance Spectroscopy-Based Studies of the Metabolism of Food-Borne Carcinogen 2-Amino-3-Methylimidazo[4,5- f ]Quinoline by Human Intestinal Microbiota

Author: Sylvie Rabot, Marja-Liisa Väisänen, Christèle Humblot, Bruno Combourieu, Jean-Pierre Furet, Anne-Marie Delort, Unité de recherche d'Écologie et Physiologie du Système Digestif (UEPSD), Institut National de la Recherche Agronomique (INRA), Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: Adult, Male, Magnetic Resonance Spectroscopy, CARCINOGEN, Mutagen, medicine.disease_cause, Applied Microbiology and Biotechnology, Microbial Ecology, Ames test, Feces, 03 medical and health sciences, Clostridium, intestin, INTESTINAL MICROBIOTA, Escherichia coli, MICROFLORE INTESTINALE, medicine, Animals, Bacteroides, Humans, Cecum, Carcinogen, 030304 developmental biology, [SDV.EE]Life Sciences [q-bio]/Ecology, environment, 0303 health sciences, Ecology, biology, 030306 microbiology, HUMAN, RAT, Clostridium perfringens, biology.organism_classification, Rats, Inbred F344, Rats, Intestines, Biochemistry, Food, Culture Media, Conditioned, Carcinogens, Quinolines, Bacteria, Food Science, Biotechnology
Abstract: 2-Amino-3-methylimidazo[4,5- f ]quinoline (IQ) is a mutagenic/carcinogenic compound formed from meat and fish during cooking. Following ingestion, IQ is metabolized mainly by liver xenobiotic-metabolizing enzymes, but intestinal bacteria may also contribute to its biotransformation. The aim of this study was to investigate the metabolism of IQ by the human intestinal microbiota. Following incubation of IQ (200 μM) under anoxic conditions with 100-fold dilutions of stools freshly collected from three healthy volunteers, we quantified residual IQ by high-pressure liquid chromatography (HPLC) analysis and characterized the production of IQ metabolites by in situ 1 H nuclear magnetic resonance ( 1 H-NMR) spectroscopic analysis of crude incubation media. In addition, we looked for IQ-degrading bacteria by screening collection strains and by isolating new strains from the cecal contents of human-microbiota-associated rats gavaged with IQ on a regular basis. HPLC and 1 H-NMR analyses showed that the three human microbiota degraded IQ with different efficiencies (range, 50 to 91% after 72 h of incubation) and converted it into a unique derivative, namely, 7-hydroxy-IQ. We found 10 bacterial strains that were able to perform this reaction: Bacteroides thetaiotaomicron ( n = 2), Clostridium clostridiiforme ( n = 3), Clostridium perfringens ( n = 1), and Escherichia coli ( n = 4). On the whole, our results indicate that bacteria belonging to the predominant communities of the human intestine are able to produce 7-hydroxy-IQ from IQ. They also suggest interindividual differences in the ability to perform this reaction. Whether it is a metabolic activation is still a matter of debate, since 7-hydroxy-IQ has been shown to be a direct-acting mutagen in the Ames assay but not carcinogenic in laboratory rodents.
Published: 2005

43. Synthesis of bridged aza-rebeccamycin analogues

Author: Michelle Prudhomme, Fabrice Anizon, Samir Messaoudi, Bruno Pfeiffer, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: Stereochemistry, Rebeccamycin, 7-Azaindole, 010402 general chemistry, 01 natural sciences, Biochemistry, chemistry.chemical_compound, Drug Discovery, medicine, Moiety, Antitumor compounds, Imide, Sugar, Indole test, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Organic Chemistry, Enzyme inhibitors, Carbohydrate, Staurosporine, 0104 chemical sciences, Pyranose, chemistry, Mitsunobu reaction, medicine.drug
Abstract: The syntheses of rebeccamycin analogues possessing a 7-azaindole moiety instead of an indole unit, and with both indole and azaindole moieties linked to the carbohydrate are described. In these bridged aza compounds, the oxygen of the pyranose heterocycle is oriented towards either the indole, or the azaindole unit. In these series, compounds bearing a free imide nitrogen were synthesized by coupling the corresponding aglycones with a sugar pre-tosylated in 2-position via a Mitsunobu reaction. To obtain a precursor for bridged aza-rebeccamycin analogues substituted in 6-position on the sugar moiety, a 2,6-ditosylated sugar was used.
Published: 2005

44. Synthesis of granulatimide bis-imide analogues

Author: Bruno Pfeiffer, Fabrice Anizon, Bernadette Hugon, Michelle Prudhomme, Samir Messaoudi, Hélène Henon, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Granulatimide, Dipyrrolo[3, Stereochemistry, 7-Azaindole, 010402 general chemistry, 01 natural sciences, Biochemistry, 6-tetraone, chemistry.chemical_compound, Drug Discovery, 4-c]carbazole-1, Moiety, Imidazole, Imide, Maleimide, Indole test, Isogranulatimide, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Chemistry, 4-g]indole-1, Organic Chemistry, Combinatorial chemistry, 3. Good health, 0104 chemical sciences, 3-b]dipyrrolo[3, 4-a:3, 4-e:3, Pyridino[2
Abstract: The synthesis of dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, structurally related to granulatimide is reported. These compounds can be considered as granulatimide analogues in which a maleimide heterocycle replaces the imidazole moiety. The synthesis of pyridino[2,3-b]dipyrrolo[3,4-e:3,4-g]indole-1,3,4,6-tetraones is also reported. In these compounds, a 7-azaindole unit replaces the indole moiety present in the granulatimide and isogranulatimide structures.
Published: 2005

45. Conformational analysis of new 14-membered ring diketal dilactam macrocycles: molecular mechanics, liquid and solid state NMR studies

Author: Denise Dugat, Bruno Combourieu, Jacques Guyot, Anne-Gaëlle Valade, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Stereochemistry, Hydrogen bond, Chemistry, Computational studies, Organic Chemistry, Stacking, Substituent, Nuclear magnetic resonance spectroscopy, 010402 general chemistry, Ring (chemistry), 01 natural sciences, Biochemistry, 0104 chemical sciences, chemistry.chemical_compound, Conformational analysis, Diketal dilactam macrocycles, Intramolecular force, Amide, Drug Discovery, Molecule, Liquid and solid state NMR
Abstract: A conformational study of new diversely substituted 14-membered diketal dilactam macrocycles was conducted by NMR spectroscopy in liquid and solid states, molecular mechanics calculations and, for one compound, a previous X-ray analysis. The results obtained by the different techniques show that the conformations depend closely on whether the molecules are chiral or achiral and on the stereochemistry of the ketal OMe groups. In achiral compounds, the most stable conformation of each compound has, in both the liquid and solid states, the two NH–CO links positioned perpendicular to the macrocycle plane, lending to the trans-7,7′–OMe macrocycles 6b and 7b a rectangular [3434]-type structure. In contrast, in chiral compounds, the most stable conformations are not the same in the liquid and solid phases. In the liquid state the conformations are set by the presence of one or two N4–H⋯O1′, N4′–H⋯O1 intramolecular hydrogen bonds that position the amide group parallel to the macrocycle plane, whereas in the solid state the amide moieties again adopt a perpendicular position which can be stabilized, when the 3-R substituent is not too bulky, by intermolecular N–H⋯O C bonds between parallel sheets, and exceptionally, in the cis-7,7′-OMe-3,3′-Ph compound 1c , by a π–π stacking effect between the phenyl groups.
Published: 2005

46. Short synthesis of new salacinol analogues and their evaluation as glycosidase inhibitors

Author: Estelle Gallienne, Jean Bolte, Mohammed Benazza, Gilles Demailly, Marielle Lemaire, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)
Subjects: Stereochemistry, chemistry.chemical_element, Erythritol, 010402 general chemistry, Ring (chemistry), 01 natural sciences, Biochemistry, chemistry.chemical_compound, Cyclic sulfate, Nucleophile, Drug Discovery, Thia-anhydroalditol, Glycoside hydrolase, Zwitterion, Sulfonium sulfate inner salt, Carbon atom, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Organic Chemistry, Glycosidase inhibitors, Diastereomer, Sulfur, 0104 chemical sciences, chemistry, Salacinol
Abstract: Versatile synthesis of some analogues of the naturally-occurring α-glucosidase inhibitor salacinol ( 1 ), involving thioanhydro alditol moieties with erythro, d , l -threo, xylo, ribo, d -arabino and d -manno configurations is described. Nucleophilic attack at the least-hindered carbon atom of an l - or d -protected erythritol cyclic sulfate by the thioanhydro alditol sulfur atom yielded the desired zwitterionic compounds. In addition, the preparation of the cyclic sulfates of 2,4-O-benzylidene- d -erythritol and 2,4-O-isopropylidene- l -erythritol was improved. Enzyme inhibition tests showed that most of the new compounds were weak but specific inhibitors, while good inhibitory activity was found for a six-membered ring analogue (β-glucosidase: Ki=16 μM).
Published: 2005

47. Conformational Rigidification via Derivatization Facilitates the Determination of Absolute Configuration Using Chiroptical Spectroscopy: A Case Study of the Chiral Alcohol endo-Borneol

Author: Frank J. Devlin, Pascale Besse, Philip J. Stephens, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Circular dichroism, Camphanes, Molecular Structure, Trimethylsilyl, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Stereochemistry, Circular Dichroism, Organic Chemistry, Molecular Conformation, Absolute configuration, Ab initio, Infrared spectroscopy, Stereoisomerism, 010402 general chemistry, 01 natural sciences, 0104 chemical sciences, chemistry.chemical_compound, chemistry, Computational chemistry, Vibrational circular dichroism, Density functional theory, Derivatization
Abstract: We demonstrate that derivatization of the OH group of endo-borneol, 1, leads to conformational rigidification. Conformational analysis (CA) of 1 and its methyl, acetate, tert-butyl, and trimethylsilyl derivatives, 2-5, is carried out using ab initio density functional theory (DFT). The number of thermally accessible stable conformations is reduced from 3 in 1, to 2 in 2, and to 1 in 3-5. Comparison of IR and vibrational circular dichroism (VCD) spectra of 1 and 3-5, calculated using DFT, to experimental spectra unambiguously confirms the DFT CA. The determination of absolute configurations (ACs) of chiral molecules via analysis of chiroptical spectra using DFT methods increases in complexity and decreases in reliability as the number of populated conformations increases. Our results for endo-borneol support the conclusion that, in the case of chiral alcohols, derivatization can lead to substantial rigidification and, as a result, significantly facilitate the determination of ACs.
Published: 2005

48. A short and versatile route to chiral spiroketal skeletons

Author: Marie-Eve Sinibaldi, Isabelle Canet, Ahmatjan Tursun, Bettina Aboab, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: chemistry.chemical_classification, Isopropylidene iodides, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Stereochemistry, Organic Chemistry, Stereoselective synthesis, Hydrazone, Sequence (biology), Spiroketals, Decane, 010402 general chemistry, 01 natural sciences, Biochemistry, 0104 chemical sciences, chemistry.chemical_compound, chemistry, Drug Discovery, Acetone, Organic chemistry, Undecane
Abstract: Different chiral spiroketal skeletons are obtained, in a versatile manner, by iterative alkylations of acetone N,N-dimethylhydrazone with iodides 2 followed by a one-pot deprotection/spirocyclization sequence. This methodology has been applied successfully to the synthesis of 1,7-dioxaspiro[5.5]undecane and 1,6-dioxaspiro[4.5]decane systems.
Published: 2005

49. Slow-binding inhibition of 2-keto-3-deoxy-6-phosphogluconate (KDPG) aldolase

Author: Casimir Blonski, Laurence Hecquet, Rémi Braga, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Time Factors, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Fructose-bisphosphate aldolase, 01 natural sciences, Biochemistry, Enamine, 03 medical and health sciences, chemistry.chemical_compound, Glyceraldehyde, Drug Discovery, Escherichia coli, Pyruvates, Molecular Biology, Aldehyde-Lyases, 030304 developmental biology, Antibacterial agent, 0303 health sciences, Schiff base, biology, 010405 organic chemistry, Spectrum Analysis, Aldolase B, Organic Chemistry, Aldolase A, Iminium, 0104 chemical sciences, Kinetics, chemistry, biology.protein, Molecular Medicine
Abstract: 2-Keto-3-deoxy-6-phosphogluconate (KDPG) aldolase is a key enzyme in the Entner–Doudoroff pathway of bacteria. It catalyzes the reversible production of KDPG from pyruvate and d -glyceraldehyde 3-phosphate through a class I Schiff base mechanism. On the basis of aldolase mechanistic pathway, various pyruvate analogues bearing β-diketo structures were designed and synthesized as potential inhibitors. Their capacity to inhibit aldolase catalyzed reaction by forming stabilized iminium ion or conjugated enamine were investigated by enzymatic kinetics and UV–vis difference spectroscopy. Depending of the substituent R (methyl or aromatic ring), a competitive or a slow-binding inhibition takes place. These results were examined on the basis of the three-dimensional structure of the enzyme.
Published: 2004

50. Synthesis of a staurosporine analogue possessing a 7-azaindole unit instead of an indole moiety

Author: Samir Messaoudi, Michelle Prudhomme, Fabrice Anizon, Bruno Pfeiffer, Roy M. Golsteyn, Synthèse et étude de systèmes à intêret biologique (SEESIB), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Institut de Recherches Servier, SERVIER, and Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Subjects: Stereochemistry, Rebeccamycin, 7-Azaindole, 010402 general chemistry, 01 natural sciences, Biochemistry, chemistry.chemical_compound, Tosyl, Drug Discovery, medicine, Nucleophilic substitution, Staurosporine, Moiety, Antitumor compounds, Indole test, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Chemistry, Organic Chemistry, Enzyme inhibitors, Carbohydrate, 0104 chemical sciences, Aglycone, medicine.drug
Abstract: The synthesis of a new staurosporine analogue possessing a 7-azaindole unit instead of an indole moiety is described. This synthesis could be achieved by coupling a sugar moiety previously tosylated in 2′ position to the azaindolocarbazole aglycone. Nucleophilic substitution on the carbon bearing the tosyl group yielded to the key cyclization leading to a compound in which the carbohydrate part is linked to both indole and azaindole nitrogens.
Published: 2004

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