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Identification of cinnamic acid derivatives as novel antagonists of the prokaryotic proton-gated ion channel GLIC

…, S Delarue-Cochin, J Marteaux, C Colas…

文献索引:Prevost, Marie S.; Delarue-Cochin, Sandrine; Marteaux, Justine; Colas, Claire; Van Renterghem, Catherine; Blondel, Arnaud; Malliavin, Therese; Corringer, Pierre-Jean; Joseph, Delphine Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4619 - 4630

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被引用次数: 12

摘要

Pentameric ligand gated ion channels (pLGICs) mediate signal transduction. The binding of an extracellular ligand is coupled to the transmembrane channel opening. So far, all known agonists bind at the interface between subunits in a topologically conserved “orthosteric site” whose amino acid composition defines the pharmacological specificity of pLGIC subtypes. A striking exception is the bacterial proton-activated GLIC protein, exhibiting an uncommon ...