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Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure.
Bay Y, Venskutonytė R, Frantsen SM, Thorsen TS, Musgaard M, Frydenvang K, Francotte P, Pirotte B, Biggin PC, Kristensen AS, Boesen T, Pickering DS, Gajhede M, Kastrup JS. Bay Y, et al. Among authors: francotte p. FEBS J. 2024 Apr;291(7):1506-1529. doi: 10.1111/febs.17046. Epub 2024 Feb 23. FEBS J. 2024. PMID: 38145505
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. 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.
Synthesis, pharmacological and structural characterization, and thermodynamic aspects of GluA2-positive allosteric modulators with a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide scaffold.
Nørholm AB, Francotte P, Olsen L, Krintel C, Frydenvang K, Goffin E, Challal S, Danober L, Botez-Pop I, Lestage P, Pirotte B, Kastrup JS. Nørholm AB, et al. Among authors: francotte p. J Med Chem. 2013 Nov 14;56(21):8736-45. doi: 10.1021/jm4012092. Epub 2013 Nov 5. J Med Chem. 2013. PMID: 24131202
41 results