Article
Investigating the state dependence of drug binding in hERG channels using a trapped-open channel phenotype.
Scientific reports - 21 Mar 2018
Thouta Samrat, Lo Garman, Grajauskas Lukas, Claydon Tom
Abstract excerpt
The hERG channel is a key player in repolarization of the cardiac action potential. Pharmacological blockade of hERG channels depletes the cardiac repolarization reserve, increasing the risk of cardiac arrhythmias. The promiscuous nature of drug interactions with hERG presents a therapeutic challenge for drug design and development. Despite considerable effort, the mechanisms of drug binding remain incompletely...
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