Referenced in: none

Automatically associated channels: Kv11.1

Title: Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation.

Authors: C Ulens, J Tytgat

Journal, date & volume: FEBS Lett., 2000 May 26 , 474, 111-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/10828461

Abstract
The S631C mutation in human ether-à-go-go-related gene (HERG) channels has previously been reported to disrupt C-type inactivation and ion-selectivity when Cys-631 is in the oxidized state. In this study, we report the relation between pharmacology and C-type inactivation for HERGS631C channels. We demonstrate that HERGS631C in its reduced state is fully blocked by 1 microM astemizole, terfenadine and dofetilide, similar to wild-type HERG channels. In contrast, oxidized HERGS631C is insensitive for these blockers. Our results suggest that an interaction with HERG channels in the inactivated state might be a common mechanism to a variety of drugs known to block HERG channels with high affinity.