Target intelligence / Profile preview

L-type calcium channel protein CaV1.2 (vascular smooth muscle variant) (CaV1.2)

Target
CaV1.2
Molecular classification
Ion channel, Voltage-gated calcium channel, Transmembrane protein complex
01

Overview

L-type calcium channel protein CaV1.2 in vascular smooth muscle cells is the principal calcium channel controlling calcium influx, which is essential for myogenic tone, contractility, transcriptional regulation, and vascular reactivity. CaV1.2 channels are high-voltage activated, composed of pore-forming α1c and auxiliary subunits, and subject to regulation by phosphorylation, auxiliary proteins, and signaling molecules. Their altered activity is implicated in diseases like hypertension and diabetes. Pharmacological blockade of these channels with calcium channel blockers (CCBs, including dihydropyridines and non-dihydropyridines) is a key strategy for treating cardiovascular diseases such as hypertension and angina, though challenges regarding selectivity and adverse effects still persist[1][5][6][7].

Other names
L-type calcium channelCaV1.2voltage-gated calcium channel (VGCC)LTCCcalcium channels of vascular smooth muscle
02

Mechanism of action

Inhibition or blockade of L-type calcium channels, reducing calcium influx\nLowering intracellular calcium concentration, promoting vasodilation, and reducing vascular tone[5][7]\nDecreased arterial resistance, reduction in blood pressure\nReduced oxygen demand, antianginal effects

03

Biological functions

Regulation of vascular smooth muscle contractionSignal transductionControl of myogenic toneTranscriptional regulationRegulation of vascular reactivityCell proliferation
04

Disease associations

HypertensionDiabetes (vascular complications)Cardiovascular disease (including atherosclerosis and angina)Vascular remodeling
05

Safety considerations

Off-target effects on cardiac muscle (e.g., heart block, bradycardia)Peripheral edemaHypotensionReflex tachycardiaNon-specificity for channel isoforms leading to variable efficacy and side effects[3][5]
06

Interacting drugs

Amlodipine

7 more in the full profile.

07

Biomarkers

Blood pressure measurement for antihypertensive efficacyVascular reactivity indicesPossibly levels of phosphorylated CaV1.2 (as proxy for downstream signaling[1][6])

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