Article
Discovery of alpha-aminoazaheterocycle-methylglyoxal adducts as a new class of high-affinity inhibitors of cystic fibrosis transmembrane conductance regulator chloride channels.
The Journal of pharmacology and experimental therapeutics - 1 Sept 2007
Routaboul Christel, Norez Caroline, Melin Patricia, Molina Marie-Carmen, Boucherle Benjamin, Bossard Florian, Noel Sabrina, Robert Renaud, Gauthier Chantal, Becq Frédéric, Décout Jean-Luc
Abstract excerpt
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 alpha-aminoazaheterocycle-methylglyoxal adducts, inhibitors of wild-type (WT) CFTR and G551D-, G1349D-, and F508del-CFTR Cl(-) channels. In whole-cell patch-clamp...
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