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1. Slip Length in Shear Flow Over a Textured Surface

Author

Elie, Nicolas, Jolly, Pascal, Lucas-Roper, Romain, and Brunetière, Noël

Subjects
Physics - Fluid Dynamics, Condensed Matter - Soft Condensed Matter
Abstract

Hydrophobic textured surfaces are studied for their low wettability and their capacity to create a 'slippery' fluid on the surface during lubrication. To this end, the flow between two parallel surfaces is numerically addressed by computing two-dimensional numerical simulations. One of the surfaces moves with a uniform rectilinear motion, while the other is fixed, with a cavity in the middle. The steady-state flow is laminar and monophasic with a low Reynolds number. The reduction of the wall shear stress caused by a vortex in the cavity, with respect to a Couette flow, looks like the creation of an equivalent slip of the fluid on the wall at a macroscopic scale.Three methods are used to calculate the slip length: one is based on the wall shear stress and the other two are based on the speed of the fluid flow. When the slip length is calculated according to these three methods, the obtained results differ. The differences show that the slip often used in the literature is a macroscopic representation of local effects that are not necessarily slippery. The speed profiles and the streamlines are then discussed, in order to propose an explanation for this difference.

Published
2024
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5. VEGFR2 and CD34 expression associated with longer survival in patients with pleural mesothelioma in the IFCT-GFPC-0701 MAPS phase 3 trial

Author

Levallet, Guénaëlle, Dubois, Fatéméh, Elie, Nicolas, Creveuil, Christian, Brosseau, Solenn, Danel, Claire, Scherpereel, Arnaud, Lantuejoul, Sylvie, Mazières, Julien, Greillier, Laurent, Audigier-Valette, Clarisse, Bergot, Emmanuel, Moro-Sibilot, Denis, Molinier, Olivier, Léna, Hervé, Monnet, Isabelle, Morin, Franck, Gounant, Valérie, and Zalcman, Gérard

Published
2023
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20. Case Report of a 31-Year-Old Woman with COVID-19 and Chorioamnionitis at 18 Weeks of Gestation with a Twin Pregnancy and an Abdominal Cerclage for Cervical Incompetence Removed by Posterior Colpotomy Approach

Author

Khaled Massoud, Daisy A., primary, Nassar, Jean, additional, Khalifeh, Joe, additional, Saad, Jacqueline C., additional, Yacoub, Stephanie F., additional, Ghanem, Joseph, additional, Sfeir, Rouphael, additional, and Anastasiadis, Elie Nicolas, additional

Published
2023
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21. Supplementary Figure 1 from Correlation between Density of CD8+ T-cell Infiltrate in Microsatellite Unstable Colorectal Cancers and Frameshift Mutations: A Rationale for Personalized Immunotherapy

Author

Maby, Pauline, primary, Tougeron, David, primary, Hamieh, Mohamad, primary, Mlecnik, Bernhard, primary, Kora, Hafid, primary, Bindea, Gabriela, primary, Angell, Helen K., primary, Fredriksen, Tessa, primary, Elie, Nicolas, primary, Fauquembergue, Emilie, primary, Drouet, Aurélie, primary, Leprince, Jérôme, primary, Benichou, Jacques, primary, Mauillon, Jacques, primary, Le Pessot, Florence, primary, Sesboüé, Richard, primary, Tuech, Jean-Jacques, primary, Sabourin, Jean-Christophe, primary, Michel, Pierre, primary, Frébourg, Thierry, primary, Galon, Jérôme, primary, and Latouche, Jean-Baptiste, primary

Published
2023
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22. Supplementary Figure 2 from Correlation between Density of CD8+ T-cell Infiltrate in Microsatellite Unstable Colorectal Cancers and Frameshift Mutations: A Rationale for Personalized Immunotherapy

Author

Maby, Pauline, primary, Tougeron, David, primary, Hamieh, Mohamad, primary, Mlecnik, Bernhard, primary, Kora, Hafid, primary, Bindea, Gabriela, primary, Angell, Helen K., primary, Fredriksen, Tessa, primary, Elie, Nicolas, primary, Fauquembergue, Emilie, primary, Drouet, Aurélie, primary, Leprince, Jérôme, primary, Benichou, Jacques, primary, Mauillon, Jacques, primary, Le Pessot, Florence, primary, Sesboüé, Richard, primary, Tuech, Jean-Jacques, primary, Sabourin, Jean-Christophe, primary, Michel, Pierre, primary, Frébourg, Thierry, primary, Galon, Jérôme, primary, and Latouche, Jean-Baptiste, primary

Published
2023
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23. Data from Correlation between Density of CD8+ T-cell Infiltrate in Microsatellite Unstable Colorectal Cancers and Frameshift Mutations: A Rationale for Personalized Immunotherapy

Author

Maby, Pauline, primary, Tougeron, David, primary, Hamieh, Mohamad, primary, Mlecnik, Bernhard, primary, Kora, Hafid, primary, Bindea, Gabriela, primary, Angell, Helen K., primary, Fredriksen, Tessa, primary, Elie, Nicolas, primary, Fauquembergue, Emilie, primary, Drouet, Aurélie, primary, Leprince, Jérôme, primary, Benichou, Jacques, primary, Mauillon, Jacques, primary, Le Pessot, Florence, primary, Sesboüé, Richard, primary, Tuech, Jean-Jacques, primary, Sabourin, Jean-Christophe, primary, Michel, Pierre, primary, Frébourg, Thierry, primary, Galon, Jérôme, primary, and Latouche, Jean-Baptiste, primary

Published
2023
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24. Supplementary Figure 3 from Correlation between Density of CD8+ T-cell Infiltrate in Microsatellite Unstable Colorectal Cancers and Frameshift Mutations: A Rationale for Personalized Immunotherapy

Author

Maby, Pauline, primary, Tougeron, David, primary, Hamieh, Mohamad, primary, Mlecnik, Bernhard, primary, Kora, Hafid, primary, Bindea, Gabriela, primary, Angell, Helen K., primary, Fredriksen, Tessa, primary, Elie, Nicolas, primary, Fauquembergue, Emilie, primary, Drouet, Aurélie, primary, Leprince, Jérôme, primary, Benichou, Jacques, primary, Mauillon, Jacques, primary, Le Pessot, Florence, primary, Sesboüé, Richard, primary, Tuech, Jean-Jacques, primary, Sabourin, Jean-Christophe, primary, Michel, Pierre, primary, Frébourg, Thierry, primary, Galon, Jérôme, primary, and Latouche, Jean-Baptiste, primary

Published
2023
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25. Supplementary Figure Legend from Correlation between Density of CD8+ T-cell Infiltrate in Microsatellite Unstable Colorectal Cancers and Frameshift Mutations: A Rationale for Personalized Immunotherapy

Author

Maby, Pauline, primary, Tougeron, David, primary, Hamieh, Mohamad, primary, Mlecnik, Bernhard, primary, Kora, Hafid, primary, Bindea, Gabriela, primary, Angell, Helen K., primary, Fredriksen, Tessa, primary, Elie, Nicolas, primary, Fauquembergue, Emilie, primary, Drouet, Aurélie, primary, Leprince, Jérôme, primary, Benichou, Jacques, primary, Mauillon, Jacques, primary, Le Pessot, Florence, primary, Sesboüé, Richard, primary, Tuech, Jean-Jacques, primary, Sabourin, Jean-Christophe, primary, Michel, Pierre, primary, Frébourg, Thierry, primary, Galon, Jérôme, primary, and Latouche, Jean-Baptiste, primary

Published
2023
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26. Supplementary Table 1 from Correlation between Density of CD8+ T-cell Infiltrate in Microsatellite Unstable Colorectal Cancers and Frameshift Mutations: A Rationale for Personalized Immunotherapy

Author

Maby, Pauline, primary, Tougeron, David, primary, Hamieh, Mohamad, primary, Mlecnik, Bernhard, primary, Kora, Hafid, primary, Bindea, Gabriela, primary, Angell, Helen K., primary, Fredriksen, Tessa, primary, Elie, Nicolas, primary, Fauquembergue, Emilie, primary, Drouet, Aurélie, primary, Leprince, Jérôme, primary, Benichou, Jacques, primary, Mauillon, Jacques, primary, Le Pessot, Florence, primary, Sesboüé, Richard, primary, Tuech, Jean-Jacques, primary, Sabourin, Jean-Christophe, primary, Michel, Pierre, primary, Frébourg, Thierry, primary, Galon, Jérôme, primary, and Latouche, Jean-Baptiste, primary

Published
2023
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27. Supplementary Table 2 from Correlation between Density of CD8+ T-cell Infiltrate in Microsatellite Unstable Colorectal Cancers and Frameshift Mutations: A Rationale for Personalized Immunotherapy

Author

Maby, Pauline, primary, Tougeron, David, primary, Hamieh, Mohamad, primary, Mlecnik, Bernhard, primary, Kora, Hafid, primary, Bindea, Gabriela, primary, Angell, Helen K., primary, Fredriksen, Tessa, primary, Elie, Nicolas, primary, Fauquembergue, Emilie, primary, Drouet, Aurélie, primary, Leprince, Jérôme, primary, Benichou, Jacques, primary, Mauillon, Jacques, primary, Le Pessot, Florence, primary, Sesboüé, Richard, primary, Tuech, Jean-Jacques, primary, Sabourin, Jean-Christophe, primary, Michel, Pierre, primary, Frébourg, Thierry, primary, Galon, Jérôme, primary, and Latouche, Jean-Baptiste, primary

Published
2023
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28. Stereology reading protocol when using quantitative histology for the determination of sexual maturity in fish ovaries

Author

Dubroca, Laurent, Elie, Nicolas, Heude-berthelin, Clothilde, Kellner, Kristell, Le Meleder, Anna, Lepoittevin, Mélanie, Martin, Valentine, Nivet, Timothe, Sauger, Carine, Villain-naud, Nadège, Dubroca, Laurent, Elie, Nicolas, Heude-berthelin, Clothilde, Kellner, Kristell, Le Meleder, Anna, Lepoittevin, Mélanie, Martin, Valentine, Nivet, Timothe, Sauger, Carine, and Villain-naud, Nadège

Abstract

This protocol was established for the evaluation of sexual maturity for exploited stock species, using quantitative histology (stereology). This document describes the reading method used on histological slides under the cross-platform QuPath. This document follows the work of different workshops that aimed to improve the compilation of data on sexual maturity. The WKMATCH (WorKshop for MATurity staging CHairs, 2012) and the WKASMSF (Workshop for Advancing Sexual Maturity Staging in Fish, 2018) defined a universal evaluation grid for sexual maturity staging of different species, including teleosteans. During the WKMATCH workshop, two main recommendations were made, underlining the need to improve and complete knowledge on sexual maturity, as well as to harmonize the practices used to determine these sexual phases. Another workshop, the WKMATHIS (WorKshop on sexual MATurity staging from HIStological tools) that took place in Caen in 2017, added new objectives : review the current knowledge on gonad histology, determine a sexual maturity scale at a cellular level, and histological studies should be made in order to improve the determination of sexual maturity on a macroscopic scale. This protocol, drawn from these workshops and their conclusions, offers guidelines on how to read histological slides through the use of stereology. As of June 2022, this protocol is linked to the MATO (MATurité Objectif des poissons par l’histologie quantitative) project, a study restricted to female gonad and the different cellular structures found inside the ovaries for different species (Pleuronectes platessa, Lepidorhombus whiffiagonis, Lepidorhombus boscii, Mullus surmuletus and Micromesistius poutassou). This protocol will present reading methods that favor an objective reading of histological slides, through stereology, and will allow less experienced readers to partake in this exercise. For a detailed description of the germinal cells, refe

Published
2023
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29. A Quantitative Histologic Analysis of Oogenesis in the Flatfish Species Pleuronectes platessa as a Tool for Fisheries Management

Author

Sauger, Carine, Quinquis, Jerome, Berthelin, Clothilde, Lepoittevin, Mélanie, Elie, Nicolas, Dubroca, Laurent, Kellner, Kristell, Sauger, Carine, Quinquis, Jerome, Berthelin, Clothilde, Lepoittevin, Mélanie, Elie, Nicolas, Dubroca, Laurent, and Kellner, Kristell

Abstract

The following paper gives a detailed description of the oogenesis cycle for the European Plaice (Pleuronectes platessa), from oogonia to post-ovulatory follicle, including ovarian follicle and zona pellucida sizes. Noteworthy particularities were the difficulty in identifying cortical alveoli due to their very small size. Quantitative histology (stereology) on histological slides was used to determine a first size at maturity for females from the English Channel, which was found to be smaller compared to the literature (19 cm). Stereology also determined a first spawning event starting in January, with a peak in February and ongoing until March. Moreover, the use of stereology showed misclassifications for individuals categorized into a maturity phase using a macroscopic visual method. Misclassifications were found with individuals that had spawned (D) but were put under the immature (A) phase, and individuals in development (B) classified under D.

Published
2023
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30. Protocoles pour l'étude histologique de gonades de poissons marins

Author

Dubroca, Laurent, Elie, Nicolas, Kellner, Kristell, Le Meleder, Anna, Parrad, Sophie, Sauger, Carine, Villain-naud, Nadège, Dubroca, Laurent, Elie, Nicolas, Kellner, Kristell, Le Meleder, Anna, Parrad, Sophie, Sauger, Carine, and Villain-naud, Nadège

Abstract

This protocol was set up under the MATO project (MATurité Objective des poissons par histologie quantitative), as part of Carine Sauger’s PhD. The MATO project, financed by IFREMER (Institut Français de Recherche pour l'Exploitation de la Mer), aims at improving the evaluation of sexual maturity stages of exploited stock species using histology paired with a stereology reading process. The present document gathers protocols used in the study of marine female fish gonads as well as the study of the different cellular structures found in ovaries at the Port-en-Bessin IFREMER laboratory. Materials used here are not always the most optimal but favor a manual approach. Most of the histological methods found in this protocol are based on methods described by Gabe, or were modified so as to answer our queries from a fisheries point of view, from the collection of fresh samples to the staining and mounting of histological slides, including inclusion in paraffin., Ce recueil de protocoles a été mis en place dans le cadre du projet MATO (MATurité Objective des poisons par histologie quantitative) et dans le cadre de la thèse de Carine Sauger. Le projet MATO financé par l’IFREMER (Institut Français de Recherche pour l’Exploitation de la Mer) a pour but d’améliorer la détermination de la maturité sexuelle chez certaines espèces en utilisant l’histologie couplé à la stéréologie. Ce présent document recueille les protocoles utilisés à la station IFREMER de Port-en-bessin pour l’étude de gonades femelles de poissons marins et des différentes structures cellulaires retrouvées dans les ovaires. Les protocoles présents détaillent les méthodes utilisées, de la récolte de l’échantillon frais jusqu’au montage de la lame histologique et sa coloration, en passant par l’inclusion dans la paraffine. Il a été mis en place de façon à favoriser une approche manuelle des méthodes d’histologie.

Published
2023
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32. Confrontation de l’examen macroscopique à l’étude radiographique, microtomographique et histologique pour la caractérisation paléopathologique de l’os immature

Author

Bédécarrats, Samuel, Bougault, Denis, Pacory, Julia, Goux, Didier, Elie, Nicolas, Naveau, Mikaël, Skeif, Hanadi, Cazin, Antoine, Lemonnier, Florian, Chapelain de Seréville-Niel, Cécile, Centre Michel de Boüard - Centre de recherches archéologiques et historiques anciennes et médiévales (CRAHAM), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU)-Centre National de la Recherche Scientifique (CNRS), Normandie Université (NU), Centre de Microscopie Appliquée à la Biologie [Caen] (CMABio3), Interactions Cellules Organismes Environnement (ICORE), Normandie Université (NU)-Normandie Université (NU)-CHU Caen, Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN)-Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN), Laboratoire de cristallographie et sciences des matériaux (CRISMAT), Normandie Université (NU)-Normandie Université (NU)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche sur les Matériaux Avancés (IRMA), Normandie Université (NU)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université de Rouen Normandie (UNIROUEN), Normandie Université (NU)-Institut national des sciences appliquées Rouen Normandie (INSA Rouen Normandie), Institut National des Sciences Appliquées (INSA)-Normandie Université (NU)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université de Rouen Normandie (UNIROUEN), Institut National des Sciences Appliquées (INSA)-Normandie Université (NU)-Institut National des Sciences Appliquées (INSA)-Centre National de la Recherche Scientifique (CNRS), Unité Support CYCERON, Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN)-Centre National de la Recherche Scientifique (CNRS), La Fabrique de patrimoines en Normandie, Groupe des Paléopathologistes de Langue Française, and European Project

Subjects
Moyen Âge, Histologie, Radiographie, Paléopathologie, [SHS.ANTHRO-BIO]Humanities and Social Sciences/Biological anthropology, Epoque Moderne, Immature, µCTscan
Abstract

International audience; Les examens paléopathologiques de sujets immatures se confrontent au caractère peu spécifique des modifications osseuses observables macroscopiquement. Afin d’aider à la caractérisation des pathologies des sujets immatures, le CRAHAM a mené de 2020 à 2022 le programme de recherche ANCESTOR en collaboration avec la plate-forme d’imagerie CYCERON, le centre de microscopie CMABio3, le laboratoire CRISMAT et en partenariat avec La Fabrique de patrimoines en Normandie. Cette recherche, financée par l’Union européenne dans le cadre du programme opérationnel FEDER/ FSE 2014-2020, avait pour objectif d’obtenir des protocoles fiables d’analyse de pathologies osseuses, de troubles de croissance et de pathologies carentielles des enfants entre 0 et 5 ans. Envisagé pour constituer une aide à une meilleure évaluation paléopathologique des populations normandes de l’Antiquité à la période moderne, ce programme a permis de constituer un référentiel ostéologique s’appuyant sur la complémentarité des examens macroscopiques, radiographiques, microtomographiques et histologiques. Par la mise en place d’un protocole descriptif standardisé, nous avons cherché à identifier le pouvoir prédictif de l’aspect de surface du périoste sur les aspects osseux visibles par radiographie, microtomographie et histologie. Pour cela, nous nous sommes appuyés sur un corpus de 39 individus décédés avant l’âge de 3 ans et inhumés dans des cimetières normands médiévaux et modernes. Les résultats montrent que les descriptions macroscopiques sont faiblement associées aux autres descriptions et que la combinaison de plusieurs méthodes d’analyse est indispensable pour établir un lien entre l’aspect de surface et les modifications tissulaires. Ces résultats permettront d’orienter les choix méthodologiques dans l’optique d’élaborer un modèle interprétatif logiciste de diagnostic utilisable par la communauté archéo-anthropologique pour l’identification de maladies ou de carences osseuses des sujets immatures.

Published
2023

34. Targeted Radiation Exposure Induces Accelerated Aortic Valve Remodeling in ApoE −/− Mice.

Author

Rucher, Guillaume, Prigent, Kevin, Simard, Christophe, Frelin, Anne-Marie, Coquemont-Guyot, Maëlle, Elie, Nicolas, Delcroix, Nicolas, Perzo, Nicolas, Guinamard, Romain, Berger, Ludovic, and Manrique, Alain

Subjects
AORTIC valve, RADIATION exposure, SINUS of valsalva, AORTIC stenosis, MAGNETIC resonance imaging
Abstract

Thoracic radiation therapy may result in accelerated atherosclerosis and in late aortic valve stenosis (AS). In this study, we assessed the feasibility of inducing radiation-induced AS using a targeted aortic valve irradiation (10 or 20 Grays) in two groups of C57Bl6/J (WT) and ApoE−/− mice compared to a control (no irradiation). Peak aortic jet velocity was evaluated by echocardiography to characterize AS. T2*-weighted magnetic resonance imaging after injection of MPIO-αVCAM-1 was used to examine aortic inflammation resulting from irradiation. A T2* signal void on valve leaflets and aortic sinus was considered positive. Valve remodeling and mineralization were assessed using von Kossa staining. Finally, the impact of radiation on cell viability and cycle from aortic human valvular interstitial cells (hVICs) was also assessed. The targeted aortic valve irradiation in ApoE−/− mice resulted in an AS characterized by an increase in peak aortic jet velocity associated with valve leaflet and aortic sinus remodeling, including mineralization process, at the 3-month follow-up. There was a linear correlation between histological findings and peak aortic jet velocity (r = 0.57, p < 0.01). In addition, irradiation was associated with aortic root inflammation, evidenced by molecular MR imaging (p < 0.01). No significant effect of radiation exposure was detected on WT animals. Radiation exposure did not affect hVICs viability and cell cycle. We conclude that targeted radiation exposure of the aortic valve in mice results in ApoE−/−, but not in WT, mice in an aortic valve remodeling mimicking the human lesions. This preclinical model could be a useful tool for future assessment of therapeutic interventions. [ABSTRACT FROM AUTHOR]

Published
2023
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39. Management of Twin Pregnancy Complications Amid COVID-19: Posterior Colpotomy Approach for Abdominal Cerclage Removal at 18 Weeks Gestation - A Case Report.

Author

Massoud, Daisy A. Khaled, Nassar, Jean, Khalifeh, Joe, Saad, Jacqueline C., Yacoub, Stephanie F., Ghanem, Joseph, Spheir, Rouphael, and Anastasiadis, Elie Nicolas

Subjects
PREGNANCY complications, MULTIPLE pregnancy, COVID-19 pandemic, PREGNANCY, MISCARRIAGE, CHORIOAMNIONITIS
Abstract

Background: Cervical incompetence and deformities contribute significantly to mid-trimester pregnancy losses and preterm births. Abdominal cerclages prevent these complications, particularly in patients with a history of failed vaginal cerclage or severe cervical deformities. However, pregnancy complications such as chorioamnionitis and fetal demise may necessitate cerclage removal. The removal methods vary, with the least invasive being the colpotomy approach, associated with lower morbidity rates than the transabdominal approach or laparoscopy. Case Report: We detail a case involving a 31-year-old woman with a twin pregnancy at 18 weeks gestation, complicated by COVID-19 and chorioamnionitis. This clinical scenario necessitated the removal of an abdominal cerclage. Given the patient's risk profile, a posterior colpotomy approach was deemed most suitable. Conclusions: The posterior colpotomy approach provided an effective and less risky method for abdominal cerclage removal in a high-risk patient. It successfully mitigated the potential complications of general anesthesia and operative risks associated with laparoscopy/laparotomy, offering optimal operative conditions. [ABSTRACT FROM AUTHOR]

Published
2023
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45. Synthesis and biological evaluation of , a compound originally described as and an inhibitor of the anti-apoptotic protein Mcl-1

Author

Justaud, Frédéric, Paysant, Hippolyte, Weiswald, Louis Bastien, Jebahi, Abdelghani, Jouanne, Marie, Elie, Nicolas, Voisin-Chiret, Anne Sophie, Roisnel, Thierry, Orione, Clement, Levoin, Nicolas, Poulain, Laurent, Gree, Rene, Institut des Sciences Chimiques de Rennes (ISCR), Université de Rennes 1 (UR1), Université de Rennes (UNIV-RENNES)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Unité de recherche interdisciplinaire pour la prévention et le traitement des cancers (ANTICIPE), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU)-CHU Caen, Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN)-Centre Régional de Lutte contre le Cancer François Baclesse [Caen] (UNICANCER/CRLC), Normandie Université (NU)-UNICANCER-Tumorothèque de Caen Basse-Normandie (TCBN)-UNICANCER-Institut National de la Santé et de la Recherche Médicale (INSERM), Centre Régional de Lutte contre le Cancer François Baclesse [Caen] (UNICANCER/CRLC), Normandie Université (NU)-UNICANCER-Tumorothèque de Caen Basse-Normandie (TCBN), Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie Université (NU)-Normandie Université (NU), Interactions Cellules Organismes Environnement (ICORE), Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN), Centre de Microscopie Appliquée à la Biologie [Caen] (CMABio3), Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN)-Université de Caen Normandie (UNICAEN), Centre Régional de Mesures Physiques de l'Ouest (CRMPO), Université de Rennes (UNIV-RENNES)-Université de Rennes (UNIV-RENNES), Bioprojet-Biotech, CNRS Centre National de la Recherche Scientifique (CNRS) European Commission, University of Rennes 1, Ligue contre le Cancer Ligue nationale contre le cancer, Conseil Interregional Grand Ouest, Ligue Contre le Cancer Ligue nationale contre le cancer, Conseil Interregional de Normandie et Comite du Calvados\', Conseil Regional de Normandie, European Union - Normandy County Council, European Union European Commission, French State (CPER Innovons 2), University of Caen Normandie, Inserm Institut National de la Sante et de la Recherche Medicale (Inserm) European Commission, and Normandy Doctoral School 497 \'EDN Bise\'

Subjects
[CHIM]Chemical Sciences
Abstract

International audience; The development of inhibitors of anti-apoptotic proteins, such as Mcl-1, is currently a very active area in the field of cancer research. One of the very first reported inhibitors of Mcl-1 was the MIM1 molecule, but we have recently demonstrated that the structure of this compound had to be revised from 2 to the derivative 1 (FJ-809). In this paper we first develop a strategy to unambiguously prepare molecules such as 1 with a thiazol-3(2H)-yl)imino core, instead of the [2(3H)-thiazolylidene]hydrazine previously found in MIM1 (2). Next a series of biological studies have been performed on 1, using IGROV1-R10 ovarian cancer cells as models, and they have been complemented by fluorescence polarisation assays. These studies demonstrated that the new compound FJ-809(1) was devoid of any significant activity on Mcl-1, in contrast to 2. Then molecular modelling and molecular dynamics studies have been performed in order to elucidate the differences between FJ-809 and MIM1 in their interaction with the Mcl-1 protein.

Published
2022

48. Synthesis and biological evaluation of FJ-809, a compound originally described as MIM1 and inhibitor of the anti-apoptotic protein Mcl-1.

Author

Justaud, Frédéric, primary, Paysant, Hippolyte, additional, Weiswald, Louis Bastien, additional, Jebahi, Abdelghani, additional, Jouanne, Marie, additional, Elie, Nicolas, additional, Voisin-Chiret, Anne Sophie, additional, Roisnel, Thierry, additional, Orione, Clément, additional, Levoin, Nicolas, additional, Poulain, Laurent, additional, and Grée, René, additional

Published
2022
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