Target intelligence / Profile preview

Short transient receptor potential channel 1 (TRPC1)

Target
TRPC1
Molecular classification
Ion channel, Transient receptor potential channel, Non-selective cation channel, TRPC subfamily
01

Overview

Short transient receptor potential channel 1 (TRPC1) is a non-selective cation channel and the first identified member of the canonical TRP channel subfamily. It is ubiquitously expressed and functions primarily as a component of store-operated calcium entry (SOCE) channels, often forming heteromeric complexes with other TRPC subunits or Orai1 (UniProt: P48967). TRPC1 plays a vital role in regulating intracellular calcium homeostasis, which is essential for processes such as cell proliferation, migration, and muscle contraction (PubMed: 28213494). In disease states, TRPC1 is frequently upregulated, contributing to the progression of various cancers, cardiac hypertrophy, and neurodegenerative conditions like Parkinson's disease (PubMed: 25100785). Pharmacological targeting of TRPC1 has been explored using inhibitors like SKF-96365 and GsMTx4, though these often lack the specificity required for clinical use (PubMed: 30144444). Consequently, TRPC1 remains a significant target for drug discovery aimed at modulating calcium-dependent signaling pathways in chronic diseases.

Other names
Transient receptor potential cation channel subfamily C member 1TRP1HTRP1Transient receptor protein 1TRPC1
02

Mechanism of action

Inhibition of non-selective cation influx and modulation of store-operated calcium entry (SOCE) to regulate intracellular calcium levels (PubMed: 28213494).

03

Biological functions

Calcium signalingStore-operated calcium entry (SOCE)Cell proliferationCell migrationMechanosensationMyogenesisVascular tone regulation
04

Disease associations

CancerCardiovascular diseaseNeurodegenerative diseaseInflammationDiabetic nephropathyMuscular dystrophy
05

Safety considerations

Potential off-target effects due to ubiquitous expression in the brain, heart, and vasculatureInterference with essential physiological calcium homeostasisLack of high selectivity in current pharmacological agents leading to cross-reactivity with other TRP channelsPotential impact on cardiac contractility and neuronal signaling
06

Interacting drugs

SKF-96365

6 more in the full profile.

07

Biomarkers

TRPC1 mRNA expression levelsTRPC1 protein expression in tissue biopsies

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