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355 results on '"Colombo, Diego"'

103. [a]C#

Author

Cazzola, Walter, primary, Cisternino, Antonio, additional, and Colombo, Diego, additional

Published
2005
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109. Inhibitory effect of stabilized analogues of glycoglycerolipids on Epstein–Barr virus activation and mouse skin tumor promotion

Author

Colombo, Diego, primary, Compostella, Federica, additional, Ronchetti, Fiamma, additional, Reza-Elahi, Shahrzad, additional, Scala, Antonio, additional, Toma, Lucio, additional, Aoi, Wataru, additional, Kuchide, Masashi, additional, Takayasu, Junko, additional, Tokuda, Harukuni, additional, and Nishino, Hoyoku, additional

Published
2002
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115. Asymmetric synthesis and preliminary evaluation of (R)- and (S)-[11C]bisoprolol, a putative β1-selective adrenoceptor radioligand

Author

Soloviev, Dmitri V., primary, Matarrese, Mario, additional, Moresco, Rosa Maria, additional, Todde, Sergio, additional, Bonasera, Thomas A., additional, Sudati, Francesco, additional, Simonelli, Pasquale, additional, Magni, Fulvio, additional, Colombo, Diego, additional, Carpinelli, Assunta, additional, Galli Kienle, Marzia, additional, and Fazio, Ferruccio, additional

Published
2001
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118. Order-Independent Constraint-Based Causal Structure Learning.

Author

Colombo, Diego and Maathuis, Marloes H.

Subjects
*GRANGER causality test, *MACHINE learning, *ALGORITHMS, *COMPUTER simulation, *YEAST genetic engineering
Abstract

We consider constraint-based methods for causal structure learning, such as the PC-, FCI-, RFCI- and CCD- algorithms (Spirtes et al., 1993, 2000; Richardson, 1996; Colombo et al., 2012; Claassen et al., 2013). The first step of all these algorithms consists of the adjacency search of the PC-algorithm. The PC-algorithm is known to be order-dependent, in the sense that the output can depend on the order in which the variables are given. This order-dependence is a minor issue in low-dimensional settings. We show, however, that it can be very pronounced in high-dimensional settings, where it can lead to highly variable results. We propose several modifications of the PC-algorithm (and hence also of the other algorithms) that remove part or all of this order-dependence. All proposed modifications are consistent in high-dimensional settings under the same conditions as their original counterparts. We compare the PC-, FCI-, and RFCI-algorithms and their modifications in simulation studies and on a yeast gene expression data set. We show that our modifications yield similar performance in low-dimensional settings and improved performance in high-dimensional settings. All software is implemented in the R-package pcalg. [ABSTRACT FROM AUTHOR]

Published
2014

120. Synthesis and Biodistribution of (R,S)-[O-Methyl-11C]-1-[3-(5-Methoxy-1,2,3,4-tetrahydro-1-naphtalenyl)propyl]-4-Phenylpiperazine (PNU-157760), A Putative Radioligand for 5-HT1AReceptors

Author

Matarrese, Mario, primary, Soloviev, Dmitrij V., additional, Moresco, Rosa M., additional, Ferri, Valentino, additional, Simonelli, Pasquale, additional, Magni, Fulvio, additional, Colombo, Diego, additional, Todde, Sergio, additional, Carpinelli, Assunta, additional, Fazio, Ferruccio, additional, and Kienle, Marzia Galli, additional

Published
1998
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122. Mono- and Disubstituted-3,8-diazabicyclo[3.2.1]octane Derivatives as Analgesics Structurally Related to Epibatidine: Synthesis, Activity, and Modeling

Author

Barlocco, Daniela, primary, Cignarella, Giorgio, additional, Tondi, Donatella, additional, Vianello, Paola, additional, Villa, Stefania, additional, Bartolini, Alessandro, additional, Ghelardini, Carla, additional, Galeotti, Nicoletta, additional, Anderson, David J., additional, Kuntzweiler, Theresa A., additional, Colombo, Diego, additional, and Toma, Lucio, additional

Published
1998
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129. Oligosaccharides related to tumor‐associate antigens. Part 3. Synthesis of the propyl glycosides of the trisaccharide β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐(1→3)‐α‐D‐Galp and of the Tetrasaccharide α‐L‐Fucp‐(1→2)‐β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐(1→3)‐α‐D‐Galp, components of a tumor antigen recognized by the antibody MBr1

Author

Lay, Luigi, primary, Panza, Luigi, additional, Russo, Giovanni, additional, Colombo, Diego, additional, Ronchetti, Fiamma, additional, Adobati, Elena, additional, and Canevari, Silvana, additional

Published
1995
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144. Vecuronium bromide and its advanced intermediates: A crystallographic and spectroscopic study.

Author

Ciceri, Samuele, Colombo, Diego, Ferraboschi, Patrizia, Grisenti, Paride, Iannone, Marco, Mori, Matteo, and Meneghetti, Fiorella

Subjects
*NEUROMUSCULAR blocking agents, *BROMIDES, *SURFACE analysis, *SKELETAL muscle, *X-ray diffraction, *ROCURONIUM bromide
Abstract

[Display omitted] • Neuromuscular blocking agents (NMBAs) induce relaxation of the skeletal muscles. • Vecuronium bromide was synthesized in higher yield, optimizing the literature synthetic process. • A complete analytical characterization of vecuronium bromide and its synthetic intermediates was reported to fill the literature gap. • Using the single-crystal X-ray diffraction (SC-XRD) technique, we unambiguously described the stereochemistry of 10 , a key intermediate for the synthesis of several NMBAs. Vecuronium bromide (Piperidinium, 1-[(2β,3α,5α,16β,17β)-3,17-bis(acetyloxy)-2-(1-piperidinyl)androstan-16-yl]-1-methyl-, bromide; Norcuron®) has been extensively used in anesthesiology practice as neuromuscular blocking agent since its launch on the market in 1982. However, a detailed crystallographic and NMR analysis of its advanced synthetic intermediates is still lacking. Hence, with the aim of filling this literature gap, vecuronium bromide was prepared starting from the commercially available 3β-hydroxy-5α-androstan-17-one (epiandrosterone), implementing some modifications to a traditional synthetic procedure. A careful NMR study allowed the complete assignment of the 1H, 13C, and 15N NMR signals of vecuronium bromide and its synthetic intermediates. The structural and stereochemical characterization of 2β,16β-bispiperidino-5α-androstane-3α,17β-diol, the first advanced synthetic intermediate carrying all the stereocenters in the final configuration, was described by means of single-crystal X-ray diffraction and Hirshfeld surface analysis, allowing a detailed conformational investigation. [ABSTRACT FROM AUTHOR]

Published
2021
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145. An Outline of the Latest Crystallographic Studies on Inhibitor-Enzyme Complexes for the Design and Development of New Therapeutics against Tuberculosis.

Author

Mori, Matteo, Villa, Stefania, Ciceri, Samuele, Colombo, Diego, Ferraboschi, Patrizia, and Meneghetti, Fiorella

Subjects
BINDING site assay, MYCOBACTERIUM tuberculosis, STRUCTURE-activity relationships, THERAPEUTICS, MULTIENZYME complexes, MYCOBACTERIAL diseases, TUBERCULOSIS
Abstract

The elucidation of the structure of enzymes and their complexes with ligands continues to provide invaluable insights for the development of drugs against many diseases, including bacterial infections. After nearly three decades since the World Health Organization's (WHO) declaration of tuberculosis (TB) as a global health emergency, Mycobacterium tuberculosis (Mtb) continues to claim millions of lives, remaining among the leading causes of death worldwide. In the last years, several efforts have been devoted to shortening and improving treatment outcomes, and to overcoming the increasing resistance phenomenon. The structural elucidation of enzyme-ligand complexes is fundamental to identify hot-spots, define possible interaction sites, and elaborate strategies to develop optimized molecules with high affinity. This review offers a critical and comprehensive overview of the most recent structural information on traditional and emerging mycobacterial enzymatic targets. A selection of more than twenty enzymes is here discussed, with a special emphasis on the analysis of their binding sites, the definition of the structure–activity relationships (SARs) of their inhibitors, and the study of their main intermolecular interactions. This work corroborates the potential of structural studies, substantiating their relevance in future anti-mycobacterial drug discovery and development efforts. [ABSTRACT FROM AUTHOR]

Published
2021
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146. Oligosaccharides related to tumor-associate antigens. Part 3. Synthesis of the propyl glycosides of the trisaccharide β- D-Galp-(1→3)-β- D-Gal pNAc-(1→3)-α- D-Gal p and of the Tetrasaccharide α- L-Fuc p-(1→2)-β- D-Gal p-(1→3)-β- D-Gal pNAc-(1→3)-α- D-Gal p, components of a tumor antigen recognized by the antibody MBr1

Author

Lay, Luigi, Panza, Luigi, Russo, Giovanni, Colombo, Diego, Ronchetti, Fiamma, Adobati, Elena, and Canevari, Silvana

Published
1995
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149. Hybrid Lipid/Polymer Nanoparticles to Tackle the Cystic Fibrosis Mucus Barrier in siRNA Delivery to the Lungs: Does PEGylation Make the Difference?

Author

Conte, Gemma, Costabile, Gabriella, Baldassi, Domizia, Rondelli, Valeria, Bassi, Rosaria, Colombo, Diego, Linardos, Giulia, Fiscarelli, Ersilia V., Sorrentino, Raffaella, Miro, Agnese, Quaglia, Fabiana, Brocca, Paola, d’Angelo, Ivana, Merkel, Olivia M., and Ungaro, Francesca

Abstract

Inhaled siRNA therapy has a unique potential for treatment of severe lung diseases, such as cystic fibrosis (CF). Nevertheless, a drug delivery system tackling lung barriers is mandatory to enhance gene silencing efficacy in the airway epithelium. We recently demonstrated that lipid-polymer hybrid nanoparticles (hNPs), comprising a poly(lactic-co-glycolic) acid (PLGA) core and a lipid shell of dipalmitoyl phosphatidylcholine (DPPC), may assist the transport of the nucleic acid cargo through mucus-covered human airway epithelium. To study in depth the potential of hNPs for siRNA delivery to the lungs and to investigate the hypothesized benefit of PEGylation, here, an siRNA pool against the nuclear factor-κB (siNFκB) was encapsulated inside hNPs, endowed with a non-PEGylated (DPPC) or a PEGylated (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol) or DSPE-PEG) lipid shell. Resulting hNPs were tested for their stability profiles and transport properties in artificial CF mucus, mucus collected from CF cells, and sputum samples from a heterogeneous and representative set of CF patients. Initial information on hNP properties governing their interaction with airway mucus was acquired by small-angle X-ray scattering (SAXS) studies in artificial and cellular CF mucus. The diffusion profiles of hNPs through CF sputa suggested a crucial role of lung colonization of the corresponding donor patient, affecting the mucin type and content of the sample. Noteworthy, PEGylation did not boost mucus penetration in complex and sticky samples, such as CF sputa from patients with polymicrobial colonization. In parallel, in vitro cell uptake studies performed on mucus-lined Calu-3 cells grown at the air–liquid interface (ALI) confirmed the improved ability of non-PEGylated hNPs to overcome mucus and cellular lung barriers. Furthermore, effective in vitroNFκB gene silencing was achieved in LPS-stimulated 16HBE14o- cells. Overall, the results highlight the potential of non-PEGylated hNPs as carriers for pulmonary delivery of siRNA for local treatment of CF lung disease. Furthermore, this study provides a detailed understanding of how distinct models may provide different information on nanoparticle interaction with the mucus barrier.

Published
2022
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150. Matrix-Assisted DOSY for Analysis of Indole Alkaloid Mixtures.

Author

You, Yu-Lin, Li, Fei-Fei, Wang, Ning, Wang, Shu-Qi, Kojima, Chojiro, and Colombo, Diego

Subjects
INDOLE alkaloids, SODIUM dodecyl sulfate, MIXTURES, SEPARATION (Technology), DIFFUSION coefficients, ISOQUINOLINE alkaloids
Abstract

Diffusion-ordered spectroscopy (DOSY) is a powerful tool for investigating mixtures and identifying peaks of chemical components. However, similar diffusion coefficients of the components, particularly for complex mixtures that contain crowded resonances, limit resolution and restrict application of the DOSY technique. In this paper, matrix-assisted DOSY were used to explore whether the diffusion resolution of a complex model involving indole alkaloid mixtures can be realized. Furthermore, we investigated the influence of different factors on the separation effect. The results showed that the changes in diffusion coefficient differences were achieved more obviously when using sodium dodecyl sulfate (SDS) micelles as the matrix. In addition, we also found that increasing the concentration of SDS can improve the resolution of the DOSY spectrum. Finally, after investigating the influence factors and NMR conditions, we demonstrated the applications of the SDS-assisted DOSY on analyzing the total alkaloid extract of Alstonia Mairei, and the virtual separation of mixtures was achieved. [ABSTRACT FROM AUTHOR]

Published
2021
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