Target intelligence / Profile preview

Human Ether-à-go-go-Related Gene potassium channel (hERG)

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

Overview

The hERG channel, encoded by the KCNH2 gene, is a voltage-gated potassium ion channel crucial for cardiac action potential repolarization. Dysfunction, either through mutations or drug blockade, leads to Long QT Syndrome (LQTS) and potentially fatal arrhythmias like torsades de pointes. Its susceptibility to blockade by a wide range of drugs poses significant safety concerns during drug development.

Other names
KCNH2Kv11.1
02

Mechanism of action

hERG channel blockade

03

Biological functions

Regulation of cardiac action potentialCell membrane repolarization
04

Disease associations

Long QT Syndrome (LQTS)Torsades de pointesSudden cardiac death
05

Safety considerations

Drug-induced QT prolongationIncreased risk of torsades de pointesPharmacological promiscuity leading to unintended blockade
06

Biomarkers

QT interval prolongation on ECG

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