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Page 1
Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target-Guided Synthesis.
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, Deprez-Poulain R. Camberlein V, et al. Among authors: gealageas r. Angew Chem Int Ed Engl. 2022 Sep 26;61(39):e202203560. doi: 10.1002/anie.202203560. Epub 2022 Aug 19. Angew Chem Int Ed Engl. 2022. PMID: 35904863 Free PMC article.
Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency.
Mpakali A, Giastas P, Deprez-Poulain R, Papakyriakou A, Koumantou D, Gealageas R, Tsoukalidou S, Vourloumis D, Mavridis IM, Stratikos E, Saridakis E. Mpakali A, et al. Among authors: gealageas r. ACS Med Chem Lett. 2017 Feb 21;8(3):333-337. doi: 10.1021/acsmedchemlett.6b00505. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337326 Free PMC article.
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity.
Bosc D, Camberlein V, Gealageas R, Castillo-Aguilera O, Deprez B, Deprez-Poulain R. Bosc D, et al. Among authors: gealageas r. J Med Chem. 2020 Apr 23;63(8):3817-3833. doi: 10.1021/acs.jmedchem.9b01183. Epub 2019 Dec 24. J Med Chem. 2020. PMID: 31820982 Review.
Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.
Hermant P, Bosc D, Piveteau C, Gealageas R, Lam B, Ronco C, Roignant M, Tolojanahary H, Jean L, Renard PY, Lemdani M, Bourotte M, Herledan A, Bedart C, Biela A, Leroux F, Deprez B, Deprez-Poulain R. Hermant P, et al. Among authors: gealageas r. J Med Chem. 2017 Nov 9;60(21):9067-9089. doi: 10.1021/acs.jmedchem.7b01444. Epub 2017 Oct 24. J Med Chem. 2017. PMID: 28985084
Development of sub-nanomolar dipeptidic ligands of neuropeptide FF receptors.
Gealageas R, Schneider S, Humbert JP, Bertin I, Schmitt M, Laboureyras E, Dugave C, Mollereau C, Simonnet G, Bourguignon JJ, Simonin F, Bihel F. Gealageas R, et al. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7471-4. doi: 10.1016/j.bmcl.2012.10.049. Epub 2012 Oct 17. Bioorg Med Chem Lett. 2012. PMID: 23131340
Development of Novel Monoamine Oxidase-B (MAO-B) Inhibitors with Reduced Blood-Brain Barrier Permeability for the Potential Management of Noncentral Nervous System (CNS) Diseases.
Gealageas R, Devineau A, So PPL, Kim CMJ, Surendradoss J, Buchwalder C, Heller M, Goebeler V, Dullaghan EM, Grierson DS, Putnins EE. Gealageas R, et al. J Med Chem. 2018 Aug 23;61(16):7043-7064. doi: 10.1021/acs.jmedchem.7b01588. Epub 2018 Aug 1. J Med Chem. 2018. PMID: 30016860