Target intelligence / Profile preview

Voltage-Gated Sodium Channel Protein Alpha Subunit (VGSC alpha subunit)

Target
VGSC alpha subunit
Molecular classification
Ion channel, Voltage-gated ion channel, Sodium channel
01

Overview

The voltage-gated sodium channel protein alpha subunit is the principal pore-forming component of voltage-gated sodium channels (VGSCs), which are essential for the initiation and propagation of action potentials in excitable cells. The alpha subunit alone is sufficient to form a functional sodium channel, but its properties can be modulated by auxiliary beta subunits. It consists of four homologous domains (I–IV), each containing six transmembrane segments (S1–S6). The S4 segment in each domain acts as the voltage sensor. Segments S5 and S6, along with the intervening pore loop, form the ion-conducting pore and activation gate. A critical intracellular loop between domains III and IV forms the fast inactivation gate. Different isoforms exist with tissue-specific expression. Mutations or dysregulation can cause "sodium channelopathies."

Other names
Sodium channel alpha subunitNav alpha subunit
02

Mechanism of action

Blocks sodium channel, preventing sodium influx and inhibiting action potential firing

03

Biological functions

Initiation of action potentialPropagation of action potentialSodium ion transportMembrane depolarization
04

Disease associations

EpilepsyCardiac arrhythmiaChronic painMyotoniaCongenital paralysisCancer
05

Safety considerations

Sodium channelopathies due to mutationsArrhythmiasSeizures
06

Interacting drugs

Local anesthetics

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