Molecular Basis of Cardiac Delayed Rectifier Potassium Channel Function and Pharmacology.

Wei Wu, Michael C Sanguinetti

Journal: Cardiac electrophysiology clinics 2017;8(2):275-84

PMID: 27261821

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Abstract

Human cardiomyocytes express 3 distinct types of delayed rectifier potassium channels. Human ether-a-go-go-related gene (hERG) channels conduct the rapidly activating current IKr; KCNQ1/KCNE1 channels conduct the slowly activating current IKs; and Kv1.5 channels conduct an ultrarapid activating current IKur. Here the authors provide a general overview of the mechanistic and structural basis of ion selectivity, gating, and pharmacology of the 3 types of cardiac delayed rectifier potassium ion channels. Most blockers bind to S6 residues that line the central cavity of the channel, whereas activators interact with the channel at 4 symmetric binding sites outside the cavity.

Address: Department of Medicine, Nora Eccles Harrison Cardiovascular Research and Training Institute, University of Utah, 95 South 2000 East, Salt Lake City, UT 84112, USA.; Department of Medicine, Nora Eccles Harrison Cardiovascular Research and Training Institute, University of Utah, 95 South 2000 East, Salt Lake City, UT 84112, USA. Electronic address: [email protected].

DOI: 10.1016/j.ccep.2016.01.002

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MeSH Terms: Delayed Rectifier Potassium Channels, Humans, Models, Molecular, Mutation, Potassium Channel Blockers