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Review
. 2008 Mar;57(3):181-95.
doi: 10.1016/j.phrs.2008.01.009. Epub 2008 Feb 2.

The hERG K+ channel: target and antitarget strategies in drug development

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Review

The hERG K+ channel: target and antitarget strategies in drug development

Emanuel Raschi et al. Pharmacol Res. 2008 Mar.

Abstract

The human ether-à-go-go related gene (hERG) K+ channel is of great interest for both basic researchers and clinicians because its blockade by drugs can lead to QT prolongation, which is a risk factor for torsades de pointes, a potentially life-threatening arrhythmia. A growing list of agents with "QT liability" have been withdrawn from the market or restricted in their use, whereas others did not even receive regulatory approval for this reason. Thus, hERG K+ channels have become a primary antitarget (i.e. an unwanted target) in drug development because their blockade causes potentially serious side effects. On the other hand, the recent identification and functional characterization of hERG K+ channels not only in the heart, but also in several other tissues (e.g. neurons, smooth muscle and cancer cells) may have far reaching implications for drug development for a possible exploitation of hERG as a target, especially in oncology and cardiology.

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