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Page 1
Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
Pizzonero M, Akkari R, Bock X, Gosmini R, De Lemos E, Duthion B, Newsome G, Mai TT, Roques V, Jary H, Lefrancois JM, Cherel L, Quenehen V, Babel M, Merayo N, Bienvenu N, Mammoliti O, Coti G, Palisse A, Cowart M, Shrestha A, Greszler S, Van Der Plas S, Jansen K, Claes P, Jans M, Gees M, Borgonovi M, De Wilde G, Conrath K. Pizzonero M, et al. Among authors: gosmini r. J Med Chem. 2024 Apr 11;67(7):5216-5232. doi: 10.1021/acs.jmedchem.3c01790. Epub 2024 Mar 25. J Med Chem. 2024. PMID: 38527911 Free PMC article.
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Temal-Laib T, Peixoto C, Desroy N, De Lemos E, Bonnaterre F, Bienvenu N, Picolet O, Sartori E, Bucher D, López-Ramos M, Roca Magadán C, Laenen W, Flower T, Mollat P, Bugaud O, Touitou R, Pereira Fernandes A, Lavazais S, Monjardet A, Borgonovi M, Gosmini R, Brys R, Amantini D, De Vos S, Andrews M. Temal-Laib T, et al. Among authors: gosmini r. J Med Chem. 2024 Jan 11;67(1):380-401. doi: 10.1021/acs.jmedchem.3c01428. Epub 2023 Dec 26. J Med Chem. 2024. PMID: 38147525 Free PMC article.
Pharmacological characterization of GLPG1972/S201086, a potent and selective small-molecule inhibitor of ADAMTS5.
Clement-Lacroix P, Little CB, Smith MM, Cottereaux C, Merciris D, Meurisse S, Mollat P, Touitou R, Brebion F, Gosmini R, De Ceuninck F, Botez I, Lepescheux L, van der Aar E, Christophe T, Vandervoort N, Blanqué R, Comas D, Deprez P, Amantini D. Clement-Lacroix P, et al. Among authors: gosmini r. Osteoarthritis Cartilage. 2022 Feb;30(2):291-301. doi: 10.1016/j.joca.2021.08.012. Epub 2021 Oct 6. Osteoarthritis Cartilage. 2022. PMID: 34626798 Free article.
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Brebion F, Gosmini R, Deprez P, Varin M, Peixoto C, Alvey L, Jary H, Bienvenu N, Triballeau N, Blanque R, Cottereaux C, Christophe T, Vandervoort N, Mollat P, Touitou R, Leonard P, De Ceuninck F, Botez I, Monjardet A, van der Aar E, Amantini D. Brebion F, et al. Among authors: gosmini r. J Med Chem. 2021 Mar 25;64(6):2937-2952. doi: 10.1021/acs.jmedchem.0c02008. Epub 2021 Mar 15. J Med Chem. 2021. PMID: 33719441 Free article.
Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.
Labéguère F, Dupont S, Alvey L, Soulas F, Newsome G, Tirera A, Quenehen V, Mai TTT, Deprez P, Blanqué R, Oste L, Le Tallec S, De Vos S, Hagers A, Vandevelde A, Nelles L, Vandervoort N, Conrath K, Christophe T, van der Aar E, Wakselman E, Merciris D, Cottereaux C, da Costa C, Saniere L, Clement-Lacroix P, Jenkins L, Milligan G, Fletcher S, Brys R, Gosmini R. Labéguère F, et al. Among authors: gosmini r. J Med Chem. 2020 Nov 25;63(22):13526-13545. doi: 10.1021/acs.jmedchem.0c00272. Epub 2020 Sep 23. J Med Chem. 2020. PMID: 32902984 Free article. Clinical Trial.
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. Gosmini R, et al. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. J Med Chem. 2014. PMID: 25249180
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
Mirguet O, Gosmini R, Toum J, Clément CA, Barnathan M, Brusq JM, Mordaunt JE, Grimes RM, Crowe M, Pineau O, Ajakane M, Daugan A, Jeffrey P, Cutler L, Haynes AC, Smithers NN, Chung CW, Bamborough P, Uings IJ, Lewis A, Witherington J, Parr N, Prinjha RK, Nicodème E. Mirguet O, et al. Among authors: gosmini r. J Med Chem. 2013 Oct 10;56(19):7501-15. doi: 10.1021/jm401088k. Epub 2013 Sep 25. J Med Chem. 2013. PMID: 24015967
BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.
Wyce A, Ganji G, Smitheman KN, Chung CW, Korenchuk S, Bai Y, Barbash O, Le B, Craggs PD, McCabe MT, Kennedy-Wilson KM, Sanchez LV, Gosmini RL, Parr N, McHugh CF, Dhanak D, Prinjha RK, Auger KR, Tummino PJ. Wyce A, et al. Among authors: gosmini rl. PLoS One. 2013 Aug 23;8(8):e72967. doi: 10.1371/journal.pone.0072967. eCollection 2013. PLoS One. 2013. PMID: 24009722 Free PMC article.
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
Mirguet O, Lamotte Y, Donche F, Toum J, Gellibert F, Bouillot A, Gosmini R, Nguyen VL, Delannée D, Seal J, Blandel F, Boullay AB, Boursier E, Martin S, Brusq JM, Krysa G, Riou A, Tellier R, Costaz A, Huet P, Dudit Y, Trottet L, Kirilovsky J, Nicodeme E. Mirguet O, et al. Among authors: gosmini r. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7. doi: 10.1016/j.bmcl.2012.01.125. Epub 2012 Feb 8. Bioorg Med Chem Lett. 2012. PMID: 22386529
12 results