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Your search keyword '"Prigent, Mathilde"' showing total 3 results
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3 results on '"Prigent, Mathilde"'

1. Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target‐Guided Synthesis

Author

Camberlein, Virgyl, primary, Fléau, Charlotte, additional, Sierocki, Pierre, additional, Li, Lenong, additional, Gealageas, Ronan, additional, Bosc, Damien, additional, Guillaume, Valentin, additional, Warenghem, Sandrine, additional, Leroux, Florence, additional, Rosell, Melissa, additional, Cheng, Keguang, additional, Medve, Laura, additional, Prigent, Mathilde, additional, Decanter, Myriam, additional, Piveteau, Catherine, additional, Biela, Alexandre, additional, Eveque, Maxime, additional, Dumont, Julie, additional, Mpakali, Anastasia, additional, Giastas, Petros, additional, Herledan, Adrien, additional, Couturier, Cyril, additional, Haupenthal, Jörg, additional, Lesire, Laetitia, additional, Hirsch, Anna K. H., additional, Deprez, Benoit, additional, Stratikos, Efstratios, additional, Bouvier, Marlene, additional, and Deprez‐Poulain, Rebecca, additional

Published
2022
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2. Discovery of the First Selective Nanomolar Inhibitors of Endoplasmic Reticulum Aminopeptidase 2 by Kinetic Target‐Guided Synthesis

Author

Camberlein, Virgyl, Fleau-Tabey, Charlotte, Sierocki, Pierre, Li, Lenong, Gealageas, Ronan, Bosc, Damien, Guillaume, Valentin, Warenghem, Sandrine, Leroux, Florence, Rosell, Melissa, Cheng, Keguang, Medve, Laura, Prigent, Mathilde, Decanter, Myriam, Piveteau, Catherine, Biela, Alexandre, Eveque, Maxime, Dumont, Julie, Mpakali, Anastasia, Giastas, Petros, Herledan, Adrien, Couturier, Cyril, Haupenthal, Jörg, Lesire, Laetitia, Hirsch, Anna, Deprez, Benoit, Stratikos, Efstratios, Bouvier, Marlene, Deprez-Poulain, Rebecca, Médicaments et molécules pour agir sur les Systèmes Vivants - U 1177 (M2SV), Institut Pasteur de Lille, Réseau International des Instituts Pasteur (RIIP)-Réseau International des Instituts Pasteur (RIIP)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Lille, University of Illinois [Chicago] (UIC), University of Illinois System, National Center for Scientific Research 'Demokritos' (NCSR), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Universität des Saarlandes [Saarbrücken], National and Kapodistrian University of Athens (NKUA), ANR-16-IDEX-0004,ULNE,ULNE(2016), and ANR-20-CE18-0003,ERAPIMM,Les inhibiteurs d'ERAP comme nouvelle approche dans le traitement des maladies autoimmunes et autoinflammatoires(2020)

Subjects
[SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences
Abstract

International audience

Published
2022

3. Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target-Guided Synthesis.

Author

Camberlein V, Fléau C, Sierocki P, Li L, Gealageas R, Bosc D, Guillaume V, Warenghem S, Leroux F, Rosell M, Cheng K, Medve L, Prigent M, Decanter M, Piveteau C, Biela A, Eveque M, Dumont J, Mpakali A, Giastas P, Herledan A, Couturier C, Haupenthal J, Lesire L, Hirsch AKH, Deprez B, Stratikos E, Bouvier M, and Deprez-Poulain R

Subjects
Histocompatibility Antigens Class I, Peptides metabolism, Aminopeptidases metabolism, Antigen Presentation
Abstract

Endoplasmic reticulum aminopeptidase 2 (ERAP2) is a key enzyme involved in the trimming of antigenic peptides presented by Major Histocompatibility Complex class I. It is a target of growing interest for the treatment of autoimmune diseases and in cancer immunotherapy. However, the discovery of potent and selective ERAP2 inhibitors is highly challenging. Herein, we have used kinetic target-guided synthesis (KTGS) to identify such inhibitors. Co-crystallization experiments revealed the binding mode of three different inhibitors with increasing potency and selectivity over related enzymes. Selected analogues engage ERAP2 in cells and inhibit antigen presentation in a cellular context. 4 d (BDM88951) displays favorable in vitro ADME properties and in vivo exposure. In summary, KTGS allowed the discovery of the first nanomolar and selective highly promising ERAP2 inhibitors that pave the way of the exploration of the biological roles of this enzyme and provide lead compounds for drug discovery efforts., (© 2022 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.)

Published
2022
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