Target intelligence / Profile preview

Voltage-gated potassium channel subunit Kv11.1 (KCNH2 (also commonly known as hERG))

Target
KCNH2 (also commonly known as hERG)
Molecular classification
Ion channel, Voltage-gated potassium channel, Membrane protein
01

Overview

The voltage-gated potassium channel subunit Kv11.1, encoded by the KCNH2 gene, forms the pore-forming alpha subunit of the hERG channel, a member of the voltage-gated potassium channel family.[1][4][3] The channel plays a critical role in the electrical repolarization of cardiac muscle after each heartbeat by mediating the rapid delayed rectifier potassium current (I_Kr), essential for maintaining a regular heart rhythm.[3][4] Each channel consists of four identical subunits with six transmembrane segments and specialized intracellular domains. Blockade or genetic mutation of Kv11.1/hERG can cause the dangerous arrhythmia "long QT syndrome," and many drugs withdrawn from the market have shown unintended hERG blockade. Beyond cardiology, KCNH2/hERG is expressed in neurons and some immune cells, and has been implicated in certain cancer cell phenotypes.[1][2][3][4]

Other names
hERGEther-à-go-go-related gene potassium channelPotassium voltage-gated channel subfamily H member 2Kv11.1
02

Mechanism of action

Blockade of the Kv11.1 (hERG) channel inhibits the IKr current, leading to prolonged repolarization phase of the cardiac action potential (lengthened QT interval). Some drugs interact as open-channel blockers. Channel agonists (less common, mainly experimental).

03

Biological functions

Cardiac action potential repolarizationRegulation of cardiac rhythmElectrical signal transmissionSignal transduction in nervous systemModulation of cell proliferation (notably in leukemic and cancer cells)
04

Disease associations

Cardiovascular disease (notably Long QT syndrome, arrhythmia, torsades de pointes, Short QT syndrome)Cancer (modulation of cancer-like features in leukemic cells)Neuropsychiatric or neurological disease (difference in neuronal function)
05

Safety considerations

Drug-induced long QT syndromeRisk of torsades de pointes (a potentially fatal ventricular tachyarrhythmia) as a consequence of hERG channel blockadeStrict regulatory scrutiny in drug development for off-target hERG interaction (hERG often considered an "antitarget")
06

Interacting drugs

Dofetilide

6 more in the full profile.

07

Biomarkers

QT interval (on ECG) as functional biomarker for hERG blockadeKCNH2/hERG expression (in some cancer cell monitoring, though not yet validated for patient selection)

Beyond the preview

Go deeper on Voltage-gated potassium channel subunit Kv11.1 (KCNH2 (also commonly known as hERG)).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Voltage-gated potassium channel subunit Kv11.1 (KCNH2 (also commonly known as hERG)).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call