Transient receptor potential cation channel subfamily V member 2 (TRPV2) (TRPV2)

Transient receptor potential cation channel subfamily V member 2 (TRPV2) is a non-selective cation channel primarily permeable to calcium and sodium ions. It belongs to the vanilloid subfamily of the transient receptor potential (TRP) channel superfamily and is widely expressed in the central nervous system, immune system, and cardiovascular tissues (UniProt Q9Y5S1). Unlike its relative TRPV1, TRPV2 is activated by noxious high temperatures exceeding 52°C and is also sensitive to mechanical stretch, osmotic stress, and various lipid signaling molecules (PubMed: 10097128). In a clinical context, TRPV2 is recognized for its significant role in cancer progression, particularly in glioblastoma, prostate cancer, and leukemia, where its overexpression correlates with increased cell proliferation and invasiveness (PubMed: 21832137). It also plays a critical role in cardiac physiology, and its dysregulation is associated with the development of dilated cardiomyopathy and muscular dystrophy (PubMed: 12644444). Pharmacologically, TRPV2 is modulated by compounds such as cannabidiol (CBD), which acts as a potent agonist, and tranilast, which serves as an inhibitor. Despite its potential as a therapeutic target for pain, inflammation, and oncology, the development of highly selective small-molecule modulators remains a primary challenge in the field.

Other names

Vanilloid receptor-like protein 1VRL-1VRL1OTRPC2VRL

Modulation of non-selective cation influx (primarily calcium and sodium) across the plasma membrane to regulate intracellular signaling, membrane potential, and cellular responses to physical or chemical stimuli.