Discovery of α-aminoazaheterocycle-methylglyoxal adducts as a new class of high-affinity inhibitors of cystic fibrosis transmembrane conductance regulator chloride …

…, F Bossard, S Noel, R Robert, C Gauthier, F Becq…

文献索引：Routaboul, Christel; Norez, Caroline; Melin, Patricia; Molina, Marie-Carmen; Boucherle, Benjamin; Bossard, Florian; Noel, Sabrina; Robert, Renaud; Gauthier, Chantal; Becq, Frederic; Decout, Jean-Luc Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 322, # 3 p. 1023 - 1035

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被引用次数: 20

摘要

Abstract The cystic fibrosis transmembrane conductance regulator (CFTR) represents the main Cl–channel in the apical membrane of epithelial cells for cAMP-dependent Cl– secretion. Here we report on the synthesis and screening of a small library of nontoxic α- aminoazaheterocycle-methylglyoxal adducts, inhibitors of wild-type (WT) CFTR and G551D-, G1349D-, and F508del-CFTR Cl–channels. In whole-cell patch-clamp experiments of ...