Activation of human ether-a-go-go related gene (hERG) potassium channels by small molecules

Ping Zheng Zhou, Joseph Babcock, Lian Qing Liu, Min Li, Zhao Bing Gao

Research output: Contribution to journalArticlepeer-review

Abstract

Human ether-a-go-go related gene (hERG) potassium (K+) channels play a critical role in cardiac action potential repolarization. Mutations that reduce hERG conductance or surface expression may cause congenital long QT syndrome (LQTS). However, the channels can be inhibited by structurally diverse small molecules, resulting in an acquired form of LQTS. Consequently, small molecules that increase the hERG current may be of value for treatment for LQTS. So far, nine hERG activators have been reported. The aim of this review is to discuss recent advances concerning the identification and action mechanism of hERG activators.

Original languageEnglish (US)
Pages (from-to)781-788
Number of pages8
JournalActa Pharmacologica Sinica
Volume32
Issue number6
DOIs
StatePublished - Jun 2011
Externally publishedYes

Keywords

  • Human ether-a-go-go related gene (hERG)
  • activator
  • ion channel
  • long QT syndrome (LQTS)

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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