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- W2074064666 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." @default.
- W2074064666 created "2016-06-24" @default.
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- W2074064666 date "2000-05-23" @default.
- W2074064666 modified "2023-10-14" @default.
- W2074064666 title "Redox state dependency of <i>HERG</i> S631C channel pharmacology: relation to C-type inactivation" @default.
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- W2074064666 doi "https://doi.org/10.1016/s0014-5793(00)01586-6" @default.
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