Target intelligence / Profile preview

Voltage-Gated Ion Channel (VGIC)

Target
VGIC
Molecular classification
Ion channel
01

Overview

Voltage-gated ion channels are a class of transmembrane proteins that form ion channels activated by changes in the electrical membrane potential across the cell membrane. These channels play a fundamental role in generating and propagating electrical signals, particularly in excitable cells such as neurons, muscle cells, and some endocrine cells. They are composed of subunits arranged to create a central pore for ion passage, including a voltage sensor, a pore domain, and a gate. These channels cycle through resting/deactivated, activated/open, and inactivated states. Different voltage-gated ion channels are selective for specific ions, including sodium, potassium, calcium, and chloride. They are essential for various physiological processes and are major drug targets due to their central role in cellular excitability.

Other names
Voltage-dependent ion channelVoltage-sensitive ion channel
02

Mechanism of action

Modulation of ion flow across the cell membrane by binding to the channel and altering its gating properties.

03

Biological functions

Initiation and propagation of action potentialsMuscle contractionHormone secretionNeuronal communicationRegulation of cellular excitability
04

Disease associations

EpilepsyCardiac arrhythmiasHypertensionNeuropathic painPsychiatric disordersChannelopathies
05

Safety considerations

Off-target effects leading to unintended consequences (e.g., cardiac effects with sodium channel blockers)Variability in patient response due to genetic polymorphisms affecting channel structure or expressionDevelopment of drug resistance through channel mutations
06

Interacting drugs

Calcium channel blockers

2 more in the full profile.

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