Target intelligence / Profile preview

KCNQ potassium channels (Kv7 channels)

Target
Kv7 channels
Molecular classification
Voltage-gated potassium channel subfamily, Kv channel subfamily
01

Overview

KCNQ potassium channels, also known as Kv7 channels, are a subfamily of voltage-gated potassium channels encoded by KCNQ genes. They are crucial regulators of cellular electrical activity by stabilizing and regulating the membrane resting potential. The family consists of five members (KCNQ1-5) forming tetrameric structures with voltage sensing and pore domains. KCNQ1 (Kv7.1) is primarily expressed in cardiac and epithelial cells, involved in cardiac repolarization and epithelial water/salt transport. KCNQ2-5 (Kv7.2-5) are mainly found in the nervous system and sensory cells, constituting the M-channel, which regulates neuronal excitability. Mutations in KCNQ genes are associated with various genetic disorders, including cardiac arrhythmias (LQTS1), deafness, epilepsy, and gastro-oesophageal adenocarcinoma. Due to their significant roles in physiological processes and disease states, KCNQ channels are considered important therapeutic targets, with modulators like activators (e.g., Retigabine) and inhibitors being developed.

Other names
Kv7 channelsKv7.1Kv7.2Kv7.3Kv7.4Kv7.5M-channel
02

Mechanism of action

Modulation of Kv7 channel activity, typically through activation or inhibition, to regulate potassium ion flow across cell membranes, thereby influencing cellular electrical excitability and membrane potential.

03

Biological functions

Regulation of cellular electrical activityStabilization and regulation of membrane resting potentialRepolarization of cardiac tissue following an action potentialWater and salt transport in epithelial tissuesFormation of delayed rectifier current IKs (KCNQ1 with KCNE1)Constituting low-threshold voltage-gated K+ channels (M-channel)Underlying the M-current (KCNQ2 and KCNQ3 heteromultimers)Potassium ion flow regulation
04

Disease associations

Cardiac arrhythmias (associated with KCNQ1 mutations)Long QT syndrome (LQTS1) (associated with KCNQ1 mutations)Deafness (associated with KCNQ1 and KCNQ4 mutations)Juvenile epilepsy (associated with KCNQ2 and KCNQ3 mutations)Gastro-oesophageal adenocarcinoma (associated with KCNQ family mutations)
05

Interacting drugs

Retigabine (activator)

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