Target intelligence / Profile preview

Transient receptor potential canonical type 6 (TRPC6)

Target: TRPC6
Molecular classification: Ion channel, Nonselective cation channel, Receptor

Overview

TRPC6 is a nonselective cation channel activated by diacylglycerol and mechanical stretch. It is widely expressed and plays key roles in vascular tone, renal filtration, and other physiological processes. Dysfunction is associated with kidney disease, pulmonary diseases, cardiac pathologies, and neurological disorders.

Mechanism of action

Agonists bind to the extracellular membrane-facing cavity formed by S6/pore helix. Antagonists bind to cytoplasmic-facing pockets within the S1-S4 domain or an intracellular membrane-facing cavity between subunits. GsMTx-4 peptide inhibits both mechanosensitive and DAG-induced activation modes.

Biological functions

Regulation of vascular toneRegulation of myogenic responseRenal filtrationCalcium signalingIon transportMechanotransduction

Disease associations

Kidney disease (focal segmental glomerulosclerosis)Pulmonary diseasesCardiac pathologiesNeurological disorders (ischemic stroke)InflammationFibrosisCancer

Safety considerations

Gain-of-function mutations can lead to kidney diseaseLoss-of-function mutations can lead to kidney diseaseCalcium overload during injury events

Interacting drugs

GsMTx-4 peptide

1 more in the full profile.

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