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Page 1
Targeting galectin-3 in inflammatory and fibrotic diseases.
Bouffette S, Botez I, De Ceuninck F. Bouffette S, et al. Among authors: botez i. Trends Pharmacol Sci. 2023 Aug;44(8):519-531. doi: 10.1016/j.tips.2023.06.001. Epub 2023 Jun 28. Trends Pharmacol Sci. 2023. PMID: 37391294 Free article. Review.
New insights in the development of positive allosteric modulators of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors belonging to 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides: Introduction of (mono/difluoro)methyl groups at the 2-position of the thiadiazine ring.
Goffin E, Fraikin P, Abboud D, de Tullio P, Beaufour C, Botez I, Hanson J, Danober L, Francotte P, Pirotte B. Goffin E, et al. Among authors: botez i. Eur J Med Chem. 2023 Mar 15;250:115221. doi: 10.1016/j.ejmech.2023.115221. Epub 2023 Feb 24. Eur J Med Chem. 2023. PMID: 36863228
Thermodynamic characterization of new positive allosteric modulators binding to the glutamate receptor A2 ligand-binding domain: combining experimental and computational methods unravels differences in driving forces.
Nørholm AB, Francotte P, Goffin E, Botez I, Danober L, Lestage P, Pirotte B, Kastrup JS, Olsen L, Oostenbrink C. Nørholm AB, et al. Among authors: botez i. J Chem Inf Model. 2014 Dec 22;54(12):3404-16. doi: 10.1021/ci500559b. Epub 2014 Dec 9. J Chem Inf Model. 2014. PMID: 25420075
Access to Galectin-3 Inhibitors from Chemoenzymatic Synthons.
Dussouy C, Téletchéa S, Lambert A, Charlier C, Botez I, De Ceuninck F, Grandjean C. Dussouy C, et al. Among authors: botez i. J Org Chem. 2020 Dec 18;85(24):16099-16114. doi: 10.1021/acs.joc.0c01927. Epub 2020 Nov 17. J Org Chem. 2020. PMID: 33200927
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: botez i. 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.
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: botez i. 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.
Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA).
Prudhomme V, Cucca M, Nauton L, Andrieu E, Fereyrolles M, Lamoine S, Michelin C, Bennis K, Collin A, De Ceuninck F, Botez I, Mallet C, Ducki S. Prudhomme V, et al. Among authors: botez i. Eur J Med Chem. 2022 Dec 15;244:114809. doi: 10.1016/j.ejmech.2022.114809. Epub 2022 Oct 1. Eur J Med Chem. 2022. PMID: 36208509
Exploring thienothiadiazine dioxides as isosteric analogues of benzo- and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators.
Francotte P, Bay Y, Goffin E, Colson T, Lesenfants C, Dorosz J, Laulumaa S, Fraikin P, de Tullio P, Beaufour C, Botez I, Pickering DS, Frydenvang K, Danober L, Kristensen AS, Kastrup JS, Pirotte B. Francotte P, et al. Among authors: botez i. Eur J Med Chem. 2024 Jan 15;264:116036. doi: 10.1016/j.ejmech.2023.116036. Epub 2023 Dec 9. Eur J Med Chem. 2024. PMID: 38101041 Free article.
11 results