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

Human Transient receptor potential cation channel subfamily C member 6 (hTRPC6) is a non-selective cation channel that primarily facilitates the influx of calcium (Ca2+) and sodium (Na+) ions into cells [1, 2, 3]. It is a member of the canonical TRP channel family and is uniquely activated by diacylglycerol (DAG) in a membrane-delimited manner, independent of protein kinase C [3, 7, 12, 20]. TRPC6 is widely expressed in tissues including the kidney, lungs, heart, and brain, where it regulates critical processes such as smooth muscle contraction, podocyte integrity in the renal slit diaphragm, and neuronal synapse formation [2, 4, 15, 18]. Gain-of-function mutations or overexpression of TRPC6 are strongly associated with focal segmental glomerulosclerosis (FSGS), pulmonary hypertension, and various malignancies, including renal and gastric cancers [1, 4, 8, 13, 16]. Conversely, its downregulation is implicated in neurodegenerative diseases like Alzheimer's and ischemic stroke [6, 14]. Therapeutic development focuses on TRPC6 antagonists, such as BI-764198 and BI 749327, for treating renal and fibrotic conditions, while activators like hyperforin are explored for neuroprotection [5, 7, 15, 17].

Other names

hTRPC6TRP6FSGS2Transient receptor potential channel 6Short transient receptor potential channel 6

TRPC6 antagonism (inhibition of cation influx) and TRPC6 agonism (activation of cation influx) [5, 6, 17]