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Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis.
Andrews MJ, Clase JA, Bar G, Tricarico G, Edwards PJ, Brys R, Chambers M, Schmidt W, MacLeod A, Hirst K, Allen V, Birault V, Le J, Harris J, Self A, Nash K, Dixon G. Andrews MJ, et al. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2266-70. doi: 10.1016/j.bmcl.2012.01.077. Epub 2012 Jan 31. Bioorg Med Chem Lett. 2012. PMID: 22342143
Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.
Van der Plas SE, Kelgtermans H, De Munck T, Martina SLX, Dropsit S, Quinton E, De Blieck A, Joannesse C, Tomaskovic L, Jans M, Christophe T, van der Aar E, Borgonovi M, Nelles L, Gees M, Stouten P, Van Der Schueren J, Mammoliti O, Conrath K, Andrews M. Van der Plas SE, et al. J Med Chem. 2018 Feb 22;61(4):1425-1435. doi: 10.1021/acs.jmedchem.7b01288. Epub 2018 Jan 10. J Med Chem. 2018. PMID: 29148763
Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis.
Van der Plas SE, Kelgtermans H, Mammoliti O, Menet C, Tricarico G, De Blieck A, Joannesse C, De Munck T, Lambin D, Cowart M, Dropsit S, Martina SLX, Gees M, Wesse AS, Conrath K, Andrews M. Van der Plas SE, et al. J Med Chem. 2021 Jan 14;64(1):343-353. doi: 10.1021/acs.jmedchem.0c01796. Epub 2021 Jan 5. J Med Chem. 2021. PMID: 33399458
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. 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.
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. 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.
Correction to "Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis".
Van der Plas SE, Kelgtermans H, Mammoliti O, Menet C, Tricarico G, De Blieck A, Joannesse C, De Munck T, Lambin D, Cowart M, Dropsit S, Martina SLX, Gees M, Wesse AS, Conrath K, Andrews M. Van der Plas SE, et al. J Med Chem. 2021 Sep 23;64(18):13933. doi: 10.1021/acs.jmedchem.1c01537. Epub 2021 Sep 14. J Med Chem. 2021. PMID: 34520202 No abstract available.
A novel, broad-spectrum inhibitor of enterovirus replication that targets host cell factor phosphatidylinositol 4-kinase IIIβ.
van der Schaar HM, Leyssen P, Thibaut HJ, de Palma A, van der Linden L, Lanke KH, Lacroix C, Verbeken E, Conrath K, Macleod AM, Mitchell DR, Palmer NJ, van de Poël H, Andrews M, Neyts J, van Kuppeveld FJ. van der Schaar HM, et al. Antimicrob Agents Chemother. 2013 Oct;57(10):4971-81. doi: 10.1128/AAC.01175-13. Epub 2013 Jul 29. Antimicrob Agents Chemother. 2013. PMID: 23896472 Free PMC article.
71 results