Article
Molecular determinants of hERG potassium channel inhibition by disopyramide.
Journal of molecular and cellular cardiology - 1 Jan 2012
El Harchi Aziza, Zhang Yi H, Hussein Leyla, Dempsey Christopher E, Hancox Jules C
Abstract excerpt
The Class Ia antiarrhythmic drug disopyramide (DISO) causes QT interval prolongation that is potentially dangerous in acquired Long QT Syndrome but beneficial in short QT syndrome, through inhibition of the hERG-encoded channels responsible for rapid delayed rectifier K(+) current (I(Kr)). In this study, alanine mutants of hERG S6 and pore helix residues and MthK-based homology modelling and ligand docking were...
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