Target intelligence / Profile preview

Potassium Channel Subfamily H Member 2 (hERG)

Target
hERG
Molecular classification
Ion channel, Potassium channel, Voltage-gated potassium channel
01

Overview

Potassium channel subfamily H member 2 (hERG) is a voltage-gated potassium ion channel encoded by the KCNH2 gene in humans. It forms the pore-forming alpha subunit of the rapid component of the delayed rectifier potassium current (I_Kr), which is essential for repolarizing cardiac action potentials and thus for normal heart rhythm. Dysfunction or inhibition leads to prolonged QT interval on ECGs—a risk factor for arrhythmias such as torsade de pointes and sudden cardiac death. Drug-induced hERG inhibition is a major concern in pharmaceutical safety testing.

Other names
Ether-à-go-go-related gene potassium channel 1Voltage-gated inwardly rectifying potassium channel KCNH2Kv11.1ERGERG1Eag homologEag-related protein 1
02

Mechanism of action

Inhibition of I_Kr current, leading to QT interval prolongation.

03

Biological functions

Cardiac repolarizationRegulation of heart rhythm
04

Disease associations

Long QT Syndrome type 2 (LQTS2)ArrhythmiaSudden cardiac death
05

Safety considerations

Drug-induced Long QT SyndromeTorsade de pointesVentricular arrhythmias
06

Interacting drugs

Astemizole

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