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Voltage-Gated Calcium Channel Alpha2delta Subunit (α2δ)
- Target
- α2δ
- Molecular classification
- Ion channel subunit, Voltage-gated calcium channel subunit, Auxiliary protein
01
Overview
The voltage-gated calcium channel alpha2delta (α2δ) subunit is an auxiliary protein component of high-voltage-activated (HVA) calcium channels, which are essential for the influx of calcium ions into excitable cells such as neurons and muscle cells upon membrane depolarization. The α2δ subunit is primarily extracellular and plays a critical role in modulating the trafficking, surface expression, and biophysical properties of the main pore-forming α1 subunit within these channels. It is targeted by drugs like gabapentin and pregabalin for the treatment of neuropathic pain and epilepsy.
- Other names
- Voltage-dependent calcium channel alpha-subunit alpha-two/deltaCACNA2D1CACNA2D2CACNA2D3CACNA2D4α2δ-1α2δ-2α2δ-3α2δ-4
02
Mechanism of action
Gabapentinoids bind to the VWA domain of α2δ subunits, primarily α2δ1 and α2δ2, modulating calcium channel activity.
03
Biological functions
Regulation of calcium ion transportModulation of calcium channel kineticsChannel traffickingSynaptic transmissionNeuronal excitabilityNeurotransmitter releaseMuscle contractionGene expressionSynaptic plasticity
04
Disease associations
Neuropathic painEpilepsyCerebellar ataxiaSpike-wave epilepsy syndromesCardiac arrhythmiasAutism spectrum disorderSchizophreniaBipolar disorderIntellectual disability syndromes
05
Interacting drugs
Gabapentin
1 more in the full profile.
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