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

Autor: 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

Publikováno v: Angewandte Chemie International Edition
Angewandte Chemie International Edition, 2022, ⟨10.1002/anie.202203560⟩

International audience

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______4254::72a3eea8d473e79d675e83d7e0715cdb
https://hal.science/hal-03754065

Modulators of hERAP2 discovered by High-Throughput Screening

Autor: Deprez Benoit, Charton Julie, Catherine Piveteau, Leroux Florence, van Endert Peter, Rosell Melissa, Deprez-Poulain Rebecca, Camberlein Virgyl, Guillaume Valentin, Castillo-Aguilera Omar, Dumont-Ryckembusch Julie, Warenghem Sandrine, Medve Laura, Fleau Charlotte, Bosc Damien, Gealageas Ronan, Lam Bao Vy

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 2020, 211, pp.113053. ⟨10.1016/j.ejmech.2020.113053⟩
European Journal of Medicinal Chemistry, Elsevier, 2020, 211, pp.113053. ⟨10.1016/j.ejmech.2020.113053⟩

International audience; Endoplasmic reticulum aminopeptidase 2, ERAP2, is an emerging pharmacological target in cancer immunotherapy and control of autoinflammatory diseases, as it is involved in antigen processing. It has been linked to the risk of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::757dddbe6404bcc4cec2bfba1545d382
https://hal.science/hal-03059990

Kinetic Target-Guided Synthesis: Reaching the Age of Maturity

Autor: Bosc, Damien, Camberlein, Virgyl, Gealageas, Ronan, Castillo-Aguilera, Omar, Deprez, Benoit, Déprez-Poulain, Rébecca

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 2019, 63 (8), pp.3817-3833. ⟨10.1021/acs.jmedchem.9b01183⟩
Journal of Medicinal Chemistry, American Chemical Society, 2019, 63 (8), pp.3817-3833. ⟨10.1021/acs.jmedchem.9b01183⟩

International audience; Kinetic target-guided synthesis (KTGS) is an original discovery strategy allowing a target to catalyze the irreversible synthesis of its own ligands from a pool of reagents. Though pioneered almost two decades ago, it only rec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::8194cb49c93bc24046fb22458d7d8302
https://hal.science/hal-03051818

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