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Voltage-dependent calcium channel auxiliary subunit alpha2delta1 (alpha2delta1)

Target: alpha2delta1
Molecular classification: Voltage-gated calcium channel subunit, Auxiliary VGCC subunit, Alpha2/Delta auxiliary VGCC subunits

Overview

The voltage-dependent calcium channel auxiliary subunit alpha2delta1 is an essential regulatory component of high-voltage activated Ca²⁺ channels encoded by the human gene CACNA2D1. It enhances surface expression/functionality of these channels while also serving as a key pharmacological target for gabapentinoid drugs used primarily in neuropathic pain management. Its broader biological roles include interactions with other neurotransmitter systems beyond classical ion channel regulation.

Other names: CACNA2D1Voltage-gated calcium channel subunit alpha2/delta-1

Mechanism of action

Binding to alpha2delta1 subunit, reducing calcium influx and modulating neurotransmitter release.

Biological functions

Regulation of calcium current densityModulation of activation/inactivation kinetics of CaV channelsTrafficking of CaV channels to the plasma membraneExcitation-contraction coupling

Disease associations

Neuropathic painEpilepsyCardiac arrhythmiasCancer

Safety considerations

Potential side effects associated with gabapentinoid drugs (e.g., dizziness, somnolence)Risk of misuse and dependence with gabapentinoids

Interacting drugs

Gabapentin

1 more in the full profile.

Biomarkers

CACNA2D1 expression in breast cancer tumor initial cells (potential)

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