hERG potassium channel and safety evaluation for drug-induced QT prolongation
Shuangqing Peng
Abstract
Shuangqing Peng
Abstract
More recent studies have shown that the K~+ channel encoded by the human ether-a- go-go related gene(hERG)as the molecular target for a wide range of drugs is associated with long-QT syndrome(LQTS)even a life-threatening form of arrhythmia known as Torsade de Points.This is major pharmacological safety concern faced by the pharmaceutical industry and the health regulation authorities. This review is about the following topics:structure and function of hERG channels;hERG channel modu- lation by differentβsubunits and cellular milieu;contemporary preclinical in vitro and in vivo methods a- bout hERG channel and drug safety evaluation and research.
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More recent studies have shown that the K~+ channel encoded by the human ether-a- go-go related gene(hERG)as the molecular target for a wide range of drugs is associated with long-QT syndrome(LQTS)even a life-threatening form of arrhythmia known as Torsade de Points.This is major pharmacological safety concern faced by the pharmaceutical industry and the health regulation authorities. This review is about the following topics:structure and function of hERG channels;hERG channel modu- lation by differentβsubunits and cellular milieu;contemporary preclinical in vitro and in vivo methods a- bout hERG channel and drug safety evaluation and research.
Key concepts: hERG, Potassium channel, Pharmacology, Long QT syndrome, QT interval, Safety pharmacology, Drug, Medicine