Molecular determinants of human ether-a-go-go-related gene 1 (hERG1) K+ channel activation by NS1643.

ABSTRACT: Human ether-à-go-go-related gene 1 (hERG1) channels conduct the rapid delayed rectifier K+ current, I(Kr), an important determinant of action potential repolarization in mammals, including humans. Reduced I(Kr) function caused by mutations in KCNH2 or drug block of hERG1 channels prolongs the QT interval of the electrocardiogram and increases the risk of ventricular fibrillation and sudden cardiac death. Several activators of hERG1 channels have been discovered in recent years. These compounds shorten the duration of cardiac action potentials and have been proposed as a new therapeutic approach for the treatment of acquired or congenital long QT syndrome. We defined previously the mechanism of action of 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643), a compound that increases h

SUBMITTER: Grunnet M 

PROVIDER: S-EPMC3014275 | biostudies-literature | 2011 Jan

REPOSITORIES: biostudies-literature