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Page 1
Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases.
Mammoliti O, Jansen K, El Bkassiny S, Palisse A, Triballeau N, Bucher D, Allart B, Jaunet A, Tricarico G, De Wachter M, Menet C, Blanc J, Letfus V, Rupčić R, Šmehil M, Poljak T, Coornaert B, Sonck K, Duys I, Waeckel L, Lecru L, Marsais F, Jagerschmidt C, Auberval M, Pujuguet P, Oste L, Borgonovi M, Wakselman E, Christophe T, Houvenaghel N, Jans M, Heckmann B, Sanière L, Brys R. Mammoliti O, et al. Among authors: jans m. J Med Chem. 2021 Oct 14;64(19):14557-14586. doi: 10.1021/acs.jmedchem.1c01066. Epub 2021 Sep 28. J Med Chem. 2021. PMID: 34581584
Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.
Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B. Joncour A, et al. Among authors: jans m. J Med Chem. 2017 Sep 14;60(17):7371-7392. doi: 10.1021/acs.jmedchem.7b00647. Epub 2017 Aug 18. J Med Chem. 2017. PMID: 28731719
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. Among authors: jans m. 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
Correction to Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2- a]pyridine Series of Autotaxin Inhibitors.
Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B. Joncour A, et al. Among authors: jans m. J Med Chem. 2018 May 10;61(9):4270. doi: 10.1021/acs.jmedchem.8b00579. Epub 2018 Apr 19. J Med Chem. 2018. PMID: 29672037 No abstract available.
Identification and Characterization of Novel CFTR Potentiators.
Gees M, Musch S, Van der Plas S, Wesse AS, Vandevelde A, Verdonck K, Mammoliti O, Hwang TC, Sonck K, Stouten P, Swensen AM, Jans M, Van der Schueren J, Nelles L, Andrews M, Conrath K. Gees M, et al. Among authors: jans m. Front Pharmacol. 2018 Oct 26;9:1221. doi: 10.3389/fphar.2018.01221. eCollection 2018. Front Pharmacol. 2018. PMID: 30416447 Free PMC article.
Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.
Mammoliti O, Palisse A, Joannesse C, El Bkassiny S, Allart B, Jaunet A, Menet C, Coornaert B, Sonck K, Duys I, Clément-Lacroix P, Oste L, Borgonovi M, Wakselman E, Christophe T, Houvenaghel N, Jans M, Heckmann B, Sanière L, Brys R. Mammoliti O, et al. Among authors: jans m. J Med Chem. 2021 May 13;64(9):6037-6058. doi: 10.1021/acs.jmedchem.1c00138. Epub 2021 May 3. J Med Chem. 2021. PMID: 33939425
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: jans m. 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.
Identification of GLPG/ABBV-2737, a Novel Class of Corrector, Which Exerts Functional Synergy With Other CFTR Modulators.
de Wilde G, Gees M, Musch S, Verdonck K, Jans M, Wesse AS, Singh AK, Hwang TC, Christophe T, Pizzonero M, Van der Plas S, Desroy N, Cowart M, Stouten P, Nelles L, Conrath K. de Wilde G, et al. Among authors: jans m. Front Pharmacol. 2019 May 9;10:514. doi: 10.3389/fphar.2019.00514. eCollection 2019. Front Pharmacol. 2019. PMID: 31143125 Free PMC article.
Arrayed adenoviral expression libraries for functional screening.
Michiels F, van Es H, van Rompaey L, Merchiers P, Francken B, Pittois K, van der Schueren J, Brys R, Vandersmissen J, Beirinckx F, Herman S, Dokic K, Klaassen H, Narinx E, Hagers A, Laenen W, Piest I, Pavliska H, Rombout Y, Langemeijer E, Ma L, Schipper C, Raeymaeker MD, Schweicher S, Jans M, van Beeck K, Tsang IR, van de Stolpe O, Tomme P, Arts GJ, Donker J. Michiels F, et al. Among authors: jans m. Nat Biotechnol. 2002 Nov;20(11):1154-7. doi: 10.1038/nbt746. Epub 2002 Sep 30. Nat Biotechnol. 2002. PMID: 12355097
Human skin stem cell-derived hepatic cells as in vitro drug discovery model for insulin-driven de novo lipogenesis.
Buyl K, Vrints M, Fernando R, Desmae T, Van Eeckhoutte T, Jans M, Van Der Schueren J, Boeckmans J, Rodrigues RM, De Boe V, Rogiers V, De Kock J, Beirinckx F, Vanhaecke T. Buyl K, et al. Among authors: jans m. Eur J Pharmacol. 2023 Oct 15;957:175989. doi: 10.1016/j.ejphar.2023.175989. Epub 2023 Aug 11. Eur J Pharmacol. 2023. PMID: 37572939 Free article.
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