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Page 1
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: de vos s, de lemos e. 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.
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, Smets B, Lepescheux L, Christophe T, Conrath K, Vandeghinste N, Vayssiere B, De Vos S, Fletcher S, Brys R, van 't Klooster G, Feyen JH, Menet C. Van Rompaey L, et al. Among authors: de vos s. J Immunol. 2013 Oct 1;191(7):3568-77. doi: 10.4049/jimmunol.1201348. Epub 2013 Sep 4. J Immunol. 2013. PMID: 24006460
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
Pizzonero M, Dupont S, Babel M, Beaumont S, Bienvenu N, Blanqué R, Cherel L, Christophe T, Crescenzi B, De Lemos E, Delerive P, Deprez P, De Vos S, Djata F, Fletcher S, Kopiejewski S, L'Ebraly C, Lefrançois JM, Lavazais S, Manioc M, Nelles L, Oste L, Polancec D, Quénéhen V, Soulas F, Triballeau N, van der Aar EM, Vandeghinste N, Wakselman E, Brys R, Saniere L. Pizzonero M, et al. Among authors: de vos s, de lemos e. J Med Chem. 2014 Dec 11;57(23):10044-57. doi: 10.1021/jm5012885. Epub 2014 Dec 1. J Med Chem. 2014. PMID: 25380412
The Medium-Chain Fatty Acid Receptor GPR84 Mediates Myeloid Cell Infiltration Promoting Steatohepatitis and Fibrosis.
Puengel T, De Vos S, Hundertmark J, Kohlhepp M, Guldiken N, Pujuguet P, Auberval M, Marsais F, Shoji KF, Saniere L, Trautwein C, Luedde T, Strnad P, Brys R, Clément-Lacroix P, Tacke F. Puengel T, et al. Among authors: de vos s. J Clin Med. 2020 Apr 16;9(4):1140. doi: 10.3390/jcm9041140. J Clin Med. 2020. PMID: 32316235 Free PMC 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: de vos s. 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.
IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases.
Lavazais S, Jargosch M, Dupont S, Labéguère F, Menet C, Jagerschmidt C, Ohm F, Kupcsik L, Parent I, Cottereaux C, Marsais F, Oste L, Van de Water A, Christophe T, De Vos S, Fallon P, Lauffer F, Clément-Lacroix P, Eyerich K, Brys R. Lavazais S, et al. Among authors: de vos s. Sci Transl Med. 2023 Feb 15;15(683):eabj3289. doi: 10.1126/scitranslmed.abj3289. Epub 2023 Feb 15. Sci Transl Med. 2023. PMID: 36791209
Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
Peixoto C, Joncour A, Temal-Laib T, Tirera A, Dos Santos A, Jary H, Bucher D, Laenen W, Pereira Fernandes A, Lavazais S, Delachaume C, Merciris D, Saccomani C, Drennan M, López-Ramos M, Wakselman E, Dupont S, Borgonovi M, Roca Magadan C, Monjardet A, Brys R, De Vos S, Andrews M, Jimenez JM, Amantini D, Desroy N. Peixoto C, et al. Among authors: de vos s. J Med Chem. 2024 Apr 11;67(7):5233-5258. doi: 10.1021/acs.jmedchem.3c02246. Epub 2024 Mar 29. J Med Chem. 2024. PMID: 38552030 Free PMC article.
Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.
Mammoliti O, Martina S, Claes P, Coti G, Blanque R, Jagerschmidt C, Shoji K, Borgonovi M, De Vos S, Marsais F, Oste L, Quinton E, López-Ramos M, Amantini D, Brys R, Jimenez JM, Galien R, van der Plas S. Mammoliti O, et al. Among authors: de vos s. J Med Chem. 2024 Jun 13;67(11):8545-8568. doi: 10.1021/acs.jmedchem.4c00769. Epub 2024 May 28. J Med Chem. 2024. PMID: 38805213 Free PMC article. Clinical Trial.
Design of a potent and selective dual JAK1/TYK2 inhibitor.
Mammoliti O, Menet C, Cottereaux C, Blanc J, De Blieck A, Coti G, Geney R, Oste L, Ostyn K, Palisse A, Quinton E, Schmitt B, Borgonovi M, Parent I, Jagerschmidt C, De Vos S, Vayssiere B, López-Ramos M, Shoji K, Brys R, Amantini D, Galien R, Joannesse C. Mammoliti O, et al. Among authors: de vos s. Bioorg Med Chem. 2024 Nov 15;114:117932. doi: 10.1016/j.bmc.2024.117932. Epub 2024 Sep 30. Bioorg Med Chem. 2024. PMID: 39447537 Free article.
250 results