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Target intelligence / Profile preview
Potassium Voltage-Gated Channel Subfamily H Member 2 (hERG)
- Target
- hERG
- Molecular classification
- Ion channel, Voltage-gated potassium channel
01
Overview
Potassium Voltage-Gated Channel Subfamily H Member 2 (hERG), also known as Kv11.1, is a voltage-dependent potassium channel crucial for cardiac action potential repolarization. Encoded by the KCNH2 gene, hERG is a tetramer forming a pore in the plasma membrane. Its unique structure, including a central cavity with hydrophobic pockets, makes it susceptible to blockade by various drugs, leading to potential cardiac arrhythmias like Long QT syndrome and Torsade de pointes. hERG contains cytoplasmic domains such as the PAS domain in the N-terminus and a cyclic nucleotide binding domain (cNBD) in the C-terminus.
- Other names
- KCNH2Eag homologEag-related protein 1ERGERG-1ERG1Ether-a-go-go-related gene potassium channel 1Ether-a-go-go-related protein 1H-ERGHERGhERG-1hERG1Voltage-gated potassium channel subunit Kv11.1
02
Mechanism of action
hERG channel blockade
03
Biological functions
Cardiac action potential repolarizationRegulation of QT intervalPotassium ion transmembrane transport
04
Disease associations
Long QT Syndrome (LQTS)Cardiac arrhythmiasTorsade de pointes
05
Safety considerations
Drug-induced Long QT SyndromeDrug-induced Torsade de pointesPotential for drug withdrawal due to hERG inhibition
06
Interacting drugs
Terfenadine
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