Target intelligence / Profile preview

Transient receptor potential canonical 4 channel (TRPC4)

Target
TRPC4
Molecular classification
Ion channel, Non-selective cation channel, Transient receptor potential channel (TRP channel)
01

Overview

Transient receptor potential canonical 4 channel (TRPC4) is a non-selective, calcium-permeable cation channel of the TRP superfamily encoded by the *TRPC4* gene. It forms homo- or heterotetrameric assemblies (e.g., with TRPC1) and is activated by receptor-coupled signaling pathways (especially Gq- and Gi-coupled receptors) as well as tyrosine kinases. TRPC4 plays key physiological roles in calcium signaling, neuronal excitability, neurotransmitter release, vascular tone, and cell proliferation. It is highly expressed in corticolimbic brain regions and endothelial cells and is implicated in neuropsychiatric disorders, epilepsy, cardiovascular regulation, and cancer biology. Experimentally, several small-molecule inhibitors and endogenous proteins (such as calmodulin) modulate TRPC4 activity, making it a potential therapeutic target in multiple disease contexts[1][3][4][5][7].

Other names
Short transient receptor potential channel 4TRP-related protein 4TRPC4Canonical TRP channel 4
02

Mechanism of action

Inhibition of channel activity (e.g., pyridazinone-based inhibitors block Ca²⁺ influx)[5]; Modulation via protein–protein interactions (e.g., CaM binding alters gating)[5]; Activation via receptor-operated (G-protein-coupled) or store-operated mechanisms

03

Biological functions

Signal transductionCalcium influx/regulationCell proliferationNeurotransmitter releaseEndothelial permeabilityVasodilation
04

Disease associations

Cardiovascular diseaseNeuropsychiatric disorders (e.g., social anxiety)Epilepsy (generalized, photosensitive)Cancer (renal cancer activity shown in preclinical studies)Other (addiction and dopamine-related processes)
05

Safety considerations

Potential off-target cardiovascular effects (due to role in vasodilation and endothelial function)Neurological/psychiatric risks (potential impact on mood, social behavior, and seizure susceptibility)Tumor progression risk (preclinical evidence in cancer models)
06

Interacting drugs

GFB-8438

3 more in the full profile.

07

Biomarkers

No specific, validated clinical biomarkers for TRPC4 patient selection or efficacy monitoring identified in current literature.

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