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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
In search of novel AMPA potentiators.
Francotte P, de Tullio P, Fraikin P, Counerotte S, Goffin E, Pirotte B. Francotte P, et al. Recent Pat CNS Drug Discov. 2006 Nov;1(3):239-46. doi: 10.2174/157488906778773661. Recent Pat CNS Drug Discov. 2006. PMID: 18221205 Review.
Coupling of liquid chromatography/tandem mass spectrometry and liquid chromatography/solid-phase extraction/NMR techniques for the structural identification of metabolites following in vitro biotransformation of SUR1-selective ATP-sensitive potassium channel openers.
Gillotin F, Chiap P, Frédérich M, Van Heugen JC, Francotte P, Lebrun P, Pirotte B, de Tullio P. Gillotin F, et al. Among authors: francotte p. Drug Metab Dispos. 2010 Feb;38(2):232-40. doi: 10.1124/dmd.109.028928. Epub 2009 Oct 29. Drug Metab Dispos. 2010. PMID: 19875500
AMPA receptor positive allosteric modulators: a patent review.
Pirotte B, Francotte P, Goffin E, de Tullio P. Pirotte B, et al. Among authors: francotte p. Expert Opin Ther Pat. 2013 May;23(5):615-28. doi: 10.1517/13543776.2013.770840. Epub 2013 Feb 13. Expert Opin Ther Pat. 2013. PMID: 23405869 Review.
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
Positive allosteric modulators of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors belonging to 4-cyclopropyl-3,4-dihydro-2h-1,2,4-pyridothiadiazine dioxides and diversely chloro-substituted 4-cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides.
Francotte P, Nørholm AB, Deva T, Olsen L, Frydenvang K, Goffin E, Fraikin P, de Tullio P, Challal S, Thomas JY, Iop F, Louis C, Botez-Pop I, Lestage P, Danober L, Kastrup JS, Pirotte B. Francotte P, et al. J Med Chem. 2014 Nov 26;57(22):9539-53. doi: 10.1021/jm501268r. Epub 2014 Nov 17. J Med Chem. 2014. PMID: 25375781
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: francotte p. 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
Synthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure-Activity Relationship at AMPA Receptors.
Larsen AP, Francotte P, Frydenvang K, Tapken D, Goffin E, Fraikin P, Caignard DH, Lestage P, Danober L, Pirotte B, Kastrup JS. Larsen AP, et al. Among authors: francotte p. ACS Chem Neurosci. 2016 Mar 16;7(3):378-90. doi: 10.1021/acschemneuro.5b00318. Epub 2016 Feb 1. ACS Chem Neurosci. 2016. PMID: 26771108
36 results