Transient receptor potential cation channel subfamily V member 6 (TRPV6) (TRPV6)

Transient receptor potential cation channel subfamily V member 6 (TRPV6) is a highly selective calcium-permeable ion channel that serves as a gatekeeper for epithelial calcium transport. It is primarily expressed in the apical membrane of the intestine and kidney, where it facilitates the absorption and reabsorption of dietary calcium to maintain systemic homeostasis (UniProt: Q9H1D0). In the context of oncology, TRPV6 is frequently overexpressed in various solid tumors, including prostate, breast, and ovarian cancers, where it promotes cell proliferation and prevents apoptosis by increasing intracellular calcium concentrations (PubMed: 29038251). Because its expression is relatively low in non-epithelial healthy tissues, it is considered a promising therapeutic target for cancer treatment. Current pharmacological strategies focus on small molecules and peptide inhibitors, such as SOR-C13, which aim to block the channel's activity and disrupt calcium-dependent oncogenic signaling (ClinicalTrials.gov: NCT01578564). However, therapeutic intervention must carefully manage potential side effects related to systemic calcium balance and bone health (PubMed: 30104345).

Other names

Calcium transport protein 1CaT1Epithelial calcium channel 2ECAC2CATLABP/TRPV6

TRPV6 inhibitors or antagonists block the pore of the channel to prevent calcium influx, thereby inhibiting calcium-dependent signaling pathways that drive tumor cell proliferation and survival.