Target intelligence / Profile preview

Voltage-dependent R-type calcium channel subunit alpha-1E (CACNA1E (also known as Cav2.3))

Target
CACNA1E (also known as Cav2.3)
Molecular classification
Ion channel, Voltage-gated calcium channel (VGCC), High-voltage activated (HVA) calcium channel
01

Overview

Voltage-dependent R-type calcium channel subunit alpha‑1E is an integral membrane protein forming the pore component of R-type voltage-gated calcium channels. Encoded by the *CACNA1E* gene (Cav2.3), it mediates high-threshold Ca²⁺ entry into neurons upon depolarization. This influx regulates diverse processes including neurotransmitter release, gene expression, cell motility, division, and death. The alpha‑1E subunit determines most biophysical properties of these channels—including their activation threshold and kinetics—and is highly expressed throughout key brain regions such as cortex and hippocampus. While less understood than other VGCCs like L-, N-, P/Q-types, emerging evidence links it to modulation of thalamocortical activity and synaptic transmission relevant for information processing in neural circuits[1][3][5].

Other names
Calcium channel, voltage-dependent, R type, alpha 1E subunitCav2.3CACNA1E
02

Mechanism of action

Drugs or molecules that interact with this protein typically act as: Channel blockers/modulators—by inhibiting the flow of Ca²⁺ through the pore formed by the alpha‑1E subunit. Modulators of neuronal excitability via alteration of action potential firing patterns.

03

Biological functions

Calcium ion import across plasma membraneSignal transduction in excitable cells (neurons)Modulation of neuronal firing patternsNeurotransmitter releaseGene expression regulationCell motility and division
04

Disease associations

Evidence suggests involvement in: Neurological disorders (e.g., epilepsy, pain syndromes)Further research may implicate it in other neuropsychiatric or neurodegenerative diseases due to its role in neuronal excitability and synaptic transmission
05

Safety considerations

Disruption of normal neuronal signaling leading to cognitive impairment, motor dysfunction, or seizures.Off-target effects on other high-voltage activated calcium channels due to structural similarity within VGCC family.These concerns are inferred from general knowledge about voltage-gated calcium channels; specific clinical data for CACNA1E inhibitors is limited.
06

Interacting drugs

No widely approved drugs specifically target the R-type/CACNA1E channels directly for clinical use.

3 more in the full profile.

07

Biomarkers

None established for patient selection or efficacy monitoring at present.

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