Article
Interactions between amiodarone and the hERG potassium channel pore determined with mutagenesis and in silico docking.
Biochemical pharmacology - 1 Aug 2016
Zhang Yihong, Colenso Charlotte K, El Harchi Aziza, Cheng Hongwei, Witchel Harry J, Dempsey Chris E, Hancox Jules C
Abstract excerpt
The antiarrhythmic drug amiodarone delays cardiac repolarisation through inhibition of hERG-encoded potassium channels responsible for the rapid delayed rectifier potassium current (IKr). This study aimed to elucidate molecular determinants of amiodarone binding to the hERG channel. Whole-cell patch-clamp recordings were made at 37°C of ionic current (IhERG) carried by wild-type (WT) or mutant hERG channels...
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