Transient receptor potential cation channel subfamily V member 5 and 6 (TRPV5/6)

Transient receptor potential cation channel subfamily V member 5 (TRPV5) and member 6 (TRPV6) are highly selective calcium channels that serve as the primary gatekeepers for epithelial calcium transport. TRPV5 is predominantly expressed in the distal convoluted tubules of the kidney, where it mediates the rate-limiting step of renal calcium reabsorption (UniProt Q9NQA5). TRPV6 is primarily localized in the intestine, facilitating the absorption of dietary calcium into the bloodstream (UniProt Q9H1D0). Together, these channels are essential for maintaining systemic calcium homeostasis, and their dysregulation is associated with metabolic bone diseases and kidney stones (IUPHAR/BPS Guide to Pharmacology). In oncology, TRPV6 is frequently overexpressed in various solid tumors, such as prostate, breast, and pancreatic cancers, where it promotes tumor progression by increasing intracellular calcium levels (PubMed: 29101247). Consequently, TRPV6 has become a therapeutic target, with inhibitors like the peptide SOR-C13 undergoing clinical trials for advanced solid tumors (ClinicalTrials.gov: NCT01578564). Monitoring calcium levels in serum and urine is critical when targeting these channels to ensure safety and efficacy.

Other names

ECaC1ECaC2CaT1Epithelial calcium channelsCalcium transport protein 1TRPV5TRPV6

Inhibition of calcium influx through the channel pore to modulate systemic calcium levels or inhibit calcium-dependent tumor cell proliferation.