Target intelligence / Profile preview

Voltage-dependent R-type calcium channel alpha-1E subunit (CaV2.3)

Target
CaV2.3
Molecular classification
Ion channel, Voltage-gated calcium channel, High-voltage activated calcium channel
01

Overview

The voltage-dependent R-type calcium channel is an ion channel responsible for mediating calcium entry into excitable cells, such as neurons and muscle cells, upon membrane depolarization[1][2][3][4][6][7]. This channel is encoded by the CACNA1E gene and forms the pore of the channel as the alpha-1E subunit (CaV2.3)[7]. R-type channels are a subtype of high-voltage-activated calcium channels, characterized by their pharmacological resistance to blockers of other subtypes (L-, N-, P/Q-type). They activate at relatively depolarized potentials and are important for neurotransmission, synaptic plasticity, and the regulation of diverse intracellular processes including gene transcription, enzymatic activity, and cell excitability[1][2][3][6]. In the nervous system, they contribute to burst firing, dendritic calcium signaling, and certain forms of synaptic transmission. Dysfunction or aberrant regulation of CaV2.3 channels has been implicated in neurological and cardiovascular disease, making them potential therapeutic targets, though clinical exploitation has been limited by the lack of highly selective drugs[6][7].

Other names
Voltage-gated R-type calcium channelR-type calcium channelCACNA1E (gene symbol)CaV2.3Voltage-sensitive calcium channel alpha-1E subunit
02

Mechanism of action

Blockade by peptide toxins (e.g. SNX-482 blocks the pore and inhibits calcium influx) - Inhibition by divalent cations (e.g. Ni^2+^, Cd^2+^) - Modulation via phosphorylation and cellular signaling pathways

03

Biological functions

Mediates calcium influx in response to membrane depolarizationRegulates neurotransmitter releaseParticipates in signal transductionInfluences gene expression, contraction, secretion, and synaptic transmissionModulates neuronal excitabilityControls enzyme activity and protein phosphorylation
04

Disease associations

Epilepsy and seizure disordersNeurodegenerative disease (roles in neuronal excitability and injury)Cardiovascular disease (linked to excitability of cardiac cells)Inflammatory disease (modulation of immune cell function)Other: roles in hormone release, pain and migraine disorders
05

Safety considerations

Potential for cardiac arrhythmia (if blocked systemically)Cognitive side effects, risk of seizure exacerbation (with indiscriminate inhibition)General risks similar to other calcium channel blockers: hypotension, bradycardia, impaired neuromuscular function
06

Interacting drugs

Ni^2+^ and Cd^2+^ ions (experimental blockers)

3 more in the full profile.

07

Biomarkers

Genetic variation in CACNA1E gene (patient selection for channelopathies)Electrophysiological properties (activation/inactivation characteristics in neurons)

Beyond the preview

Go deeper on Voltage-dependent R-type calcium channel alpha-1E subunit (CaV2.3).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Voltage-dependent R-type calcium channel alpha-1E subunit (CaV2.3).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call