Transient receptor potential vanilloid type 2 (TRPV2)

Transient receptor potential vanilloid type 2 (TRPV2) is a tetrameric, non-selective cation channel permeable to Ca²⁺ and other cations, belonging to the vanilloid (TRPV) subfamily of the transient receptor potential (TRP) superfamily. TRPV2 is expressed broadly across tissues including heart, immune cells, pancreas, nervous system, and others, and regulates diverse cellular functions such as calcium signaling, immune activation, placental development, and cell membrane dynamics. It differs from the closely related TRPV1 in its insensitivity to heat and vanilloids and its predominant localization to intracellular membranes. TRPV2 is a promising therapeutic target in cancer, cardiovascular, immune-mediated, and infectious diseases, with several small molecule modulators identified (e.g., 2-APB, probenecid, CBD). Alterations in TRPV2 function can affect disease progression and treatment outcomes, but therapeutic modulation must balance efficacy with risks linked to its critical physiological roles.

Other names

TRPV2Transient receptor potential vanilloid 2TRPV2 channelTransient receptor potential channel vanilloid subtype 2

Small molecule activators (2-APB, CBD, probenecid) bind at specific sites and cause conformational changes leading to channel opening and altered ion permeability; Inhibitors (ruthenium red, gadolinium) block channel activity; Synergistic activation (CBD + 2-APB can enhance channel opening)