Molecular Basis of Cardiac Delayed Rectifier Potassium Channel Function and Pharmacology

Publication date: Available online 18 March 2016 Source:Cardiac Electrophysiology Clinics Author(s): Wei Wu, Michael C. SanguinettiTeaser 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 I Kr; KCNQ1/KCNE1 channels conduct the slowly activating current I Ks; and Kv1.5 channels conduct an ultrarapid activating current I Kur. 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.
Source: Cardiac Electrophysiology Clinics - Category: Cardiology Source Type: research