Transient receptor potential vanilloid 6 channel (TRPV6)

Transient receptor potential vanilloid 6 channel (TRPV6) is a highly calcium-selective ion channel of the TRP family, primarily expressed in epithelial tissues (such as intestine, kidney, placenta, exocrine glands, and reproductive organs) where it mediates transcellular calcium uptake[2][4][5]. Functionally, it forms a tetrameric channel that permits calcium influx in response to physiological demand, regulated by factors including intracellular calcium, calmodulin, and lipid interactions[1]. It is essential for systemic calcium balance, bone mineralization, and reproductive health. TRPV6 is implicated in numerous pathologies, most notably cancer—where it is overexpressed in aggressive tumors—and inherited disorders of calcium transport[5]. Pharmacological inhibition of TRPV6 is under exploration for anticancer therapy, but may pose risks related to fundamental calcium homeostasis[1][5][7].

Other names

TRPV6ECaC2 (epithelial calcium channel 2)CaT1 (calcium transport protein 1)CatL (calcium channel, epithelial, involved in absorption)

Channel blockade by small molecules (e.g., 2-APB, ruthenium red, PCHPDs, econazole) leads to inhibition of calcium influx[3][7]. Competitive antagonism with endogenous regulators (e.g., calmodulin-mediated inactivation by calcium binding)[1]. Allosteric modulation via binding at S1–S4 transmembrane bundle or selectivity filter[3][7].