Target intelligence / Profile preview

Transient receptor potential cation channel subfamily C member 6 (TRPC6)

Target
TRPC6
Molecular classification
Ion channel, Receptor-activated non-selective cation channel, Transient receptor potential (TRP) channel family, classical (TRPC) subfamily
01

Overview

Transient receptor potential cation channel subfamily C member 6 (TRPC6) is a nonselective cation channel predominantly permeable to calcium ions but also capable of transporting other divalent metal ions such as zinc. It is activated directly by diacylglycerol—a product of phospholipase C activity—and plays key roles in cellular depolarization, signal transduction pathways involving intracellular Ca²⁺ elevation, regulation of vascular smooth muscle contraction/myogenic tone, synaptic development in neurons, and various physiological processes across multiple tissues. Mutations or dysregulation are implicated in several human diseases including kidney disorders like focal segmental glomerulosclerosis, cardiovascular pathologies such as hypertension/preeclampsia, and neurological conditions including epilepsy and autism spectrum disorder. Structural studies have revealed distinct binding sites for pharmacological modulators that could be exploited for therapeutic intervention.

Other names
Transient receptor potential canonical 6TRPC6
02

Mechanism of action

Drugs targeting this molecule act primarily by modulating the opening or closing of the nonselective cation channel—either inhibiting or activating calcium influx through direct binding to specific sites on the protein. Antagonists bind to a cytoplasm-facing pocket formed by S1-S4 and the TRP helix; agonists wedge at a subunit interface between S6 and the pore helix.

03

Biological functions

Signal transductionCalcium influx and homeostasisRegulation of vascular tone (myogenic response)Synapse development and neuronal signalingZinc ion transport
04

Disease associations

Cardiovascular disease (e.g., hypertension, preeclampsia)Renal disease (e.g., focal segmental glomerulosclerosis)Neurological disorders (implicated in epilepsy, autism spectrum disorders)Other diseases involving calcium signaling dysregulation
05

Safety considerations

Disruption of normal vascular tone regulation leading to blood pressure abnormalitiesAltered neuronal excitability with possible neuropsychiatric effectsImpaired renal function due to excessive or insufficient calcium influx
06

Interacting drugs

Specific small-molecule modulators (agonists and antagonists) identified in structural studies

2 more in the full profile.

07

Biomarkers

Mutations in TRPC6 (e.g., for familial focal segmental glomerulosclerosis)Altered TRPC6 expression levels (e.g., for cardiovascular risk stratification or neurological conditions)

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