Target intelligence / Profile preview

Transient receptor potential cation channel subfamily C member 4 (TRPC4)

Target
TRPC4
Molecular classification
Ion channel, TRP channel, Cation channel
01

Overview

Transient receptor potential cation channel subfamily C member 4 (TRPC4) is a non-selective, calcium-permeable cation channel involved in various physiological processes. It is activated by Gαi-coupled receptors, Gαq-coupled receptors, and tyrosine kinases, playing roles in endothelial permeability, vasodilation, neurotransmitter release, and cell proliferation. TRPC4 is highly expressed in cortico-limbic regions of the brain and endothelial cells. Its dysregulation is implicated in several diseases, including pulmonary hypertension, cardiac hypertrophy and seizure susceptibility. The channel is regulated by endogenous proteins such as calmodulin and can be modulated by small molecule inhibitors like GFB compounds.

Other names
HTRP-4HTRP4TRP4
02

Mechanism of action

Inhibition of TRPC4 channel activity

03

Biological functions

Ion transportCalcium signalingRegulation of endothelial permeabilityVasodilationNeurotransmitter releaseCell proliferation
04

Disease associations

Pulmonary hypertensionCardiac hypertrophyPodocyte injurySeizure susceptibilityFear responseGastrointestinal motility disorders
05

Interacting drugs

GFB compounds

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