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XB-ART-10939
FEBS Lett 2000 May 26;4741:111-5.
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Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation.

Ulens C , Tytgat J .


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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.

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Species referenced: Xenopus
Genes referenced: gnao1 kcnh2