Transient receptor potential vanilloid 6 (TRPV6) (TRPV6)

Transient receptor potential vanilloid 6 (TRPV6) is a highly calcium-selective, constitutively active ion channel that serves as a primary gatekeeper for systemic calcium homeostasis (NIH, 2024). It is predominantly expressed in the apical membranes of epithelial tissues, including the intestine and kidney, where it facilitates transcellular calcium absorption and reabsorption (ResearchGate, 2020). Beyond its physiological roles, TRPV6 is frequently overexpressed in various epithelial-derived malignancies, such as prostate, breast, ovarian, and pancreatic cancers, earning it the designation of an 'oncochannel' (Journal of Cancer, 2018). Its upregulation leads to sustained elevations in intracellular calcium, which activate downstream signaling pathways like the NFAT pathway to promote tumor cell proliferation, survival, and metastasis (NIH, 2024). Consequently, TRPV6 has emerged as a promising therapeutic target in oncology, with inhibitors like the peptide SOR-C13 demonstrating safety and preliminary efficacy in clinical trials (Columbia University, 2020). Therapeutic challenges include managing potential side effects related to calcium imbalance, such as hypercalciuria and impacts on bone density (NIH, 2022). Monitoring TRPV6 expression levels can serve as a biomarker for patient selection and treatment response in these cancer types (NIH, 2024).

Other names

CaT1CATLECAC2ABP/PBPCalcium transport protein 1Calcium transporter-like proteinEpithelial apical membrane calcium transporter/channel CaT1Epithelial calcium channel 2Transient receptor potential cation channel subfamily V member 6

TRPV6 inhibitors typically act by blocking the ion channel pore or inducing an inactivation-mimicking state, thereby preventing the influx of calcium ions required for tumor cell signaling and proliferation (Columbia University, 2020; NIH, 2024). Some agents may also downregulate the expression of the TRPV6 gene (NIH, 2018).