Target intelligence / Profile preview

Voltage-gated potassium channel (Kv channel) (Kv channel)

Target
Kv channel
Molecular classification
Ion channel, Voltage-gated ion channel
01

Overview

Voltage-gated potassium (Kv) channels are a diverse superfamily of transmembrane proteins that play a fundamental role in controlling the electrical excitability of cells [1]. They function by selectively conducting potassium ions across the cell membrane in response to changes in the membrane potential, primarily facilitating the repolarization phase of action potentials in neurons and muscle cells [2]. Beyond electrical signaling, these channels are involved in regulating cell volume, neurotransmitter release, and heart rate [3]. Dysfunction of Kv channels, often due to genetic mutations or autoantibodies, is linked to a variety of conditions known as channelopathies, including cardiac arrhythmias (such as Long QT Syndrome), epilepsy, and episodic ataxia [4]. Pharmacologically, they are significant targets; for instance, class III antiarrhythmics block specific Kv channels to prolong the cardiac action potential, while other modulators are used to treat multiple sclerosis and neuropathic pain [5]. However, the structural conservation across the Kv family presents a major challenge for drug development, as off-target inhibition—particularly of the hERG channel—can lead to life-threatening cardiac side effects [6]. Sources: [1] Gutman GA, et al. (2005). Pharmacological Reviews. PMID: 16330684. [2] StatPearls. (2023). Physiology, Potassium Channels. [3] Wulff H, et al. (2009). Nature Reviews Drug Discovery. PMID: 19949401. [4] Kim J. (2014). Journal of the Korean Neurological Association. [5] PubChem. (2024). Compound Summaries for Amiodarone and Fampridine. [6] Sanguinetti MC, Tristani-Firouzi M. (2006). Nature. PMID: 16554806.

Other names
Voltage-dependent potassium channelVoltage-gated K+ channelKvKCN familyPotassium voltage-gated channel
02

Mechanism of action

Drugs targeting these channels typically act as pore blockers to inhibit ion flow or as gating modifiers that shift the voltage-dependence of activation or inactivation [3, 5].

03

Biological functions

Action potential repolarization [1]Resting membrane potential maintenance [2]Neurotransmitter release regulation [3]Cardiac rhythm regulation [4]Cell volume regulation [1]
04

Disease associations

Cardiac arrhythmia [6]Epilepsy [4]Ataxia [4]Neuropathic pain [3]Multiple sclerosis [5]Diabetes [3]
05

Safety considerations

Pro-arrhythmic risk (Torsades de Pointes) [6]Seizure risk [4]Neurotoxicity [4]Off-target cardiac effects [6]
06

Interacting drugs

Amiodarone [5]

6 more in the full profile.

07

Biomarkers

QT interval prolongation [6]Serum potassium levels [2]KCNH2 mutation status [6]KCNQ1 mutation status [6]

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