Human ether-à-go-go–related gene potassium channel (Kv11.1) (hERG1 (also known as Kv11.1))

The human ether-à-go-go–related gene potassium channel (Kv11.1; hERG1), encoded by the KCNH2 gene, is a voltage-gated potassium ion channel primarily responsible for the rapid component of the delayed rectifier potassium current (I_Kr) in cardiac myocytes. This channel plays a critical role in repolarization of the cardiac action potential, preventing arrhythmogenic premature depolarizations. The hERG1 channel is a tetrameric membrane protein with each subunit containing six transmembrane domains, assembling to form the selective aqueous pore. Inherited or drug-induced dysfunction of hERG1 leads to prolongation of the QT interval, predisposing to ventricular arrhythmias and sudden cardiac death (long QT syndrome). hERG1 is also expressed in various tumor cells, where it may influence cell proliferation and apoptosis, making it a potential biomarker or therapeutic target in oncology. The channel is notable for its high susceptibility to blockade by many structurally diverse drugs, which presents significant safety concerns in drug development[2][3][4][6].

Other names

hERG1Kv11.1KCNH2Human ether-à-go-go–related gene potassium channelEther-à-go-go channel

Blockade of the hERG1 channel by drugs leads to prolongation of cardiac repolarization (QT interval) by inhibiting I_Kr current[2][3] Some activators (e.g., RPR260243) enhance channel activity by altering channel gating[5]