Transient receptor potential vanilloid 2 (TRPV2); Transient receptor potential vanilloid 3 (TRPV3) (TRPV2, TRPV3)

Transient receptor potential vanilloid 2 and 3 are members of the TRP superfamily of calcium-permeable nonselective cation channels. Both form tetrameric membrane proteins with six transmembrane domains and are distantly related to voltage-gated ion channels. - TRPV2 is widely expressed (heart, immune system, pancreas, CNS, prostate, placenta) and is implicated in cellular calcium signaling in response to extreme heat (> 52 °C), mechanical stretch, cannabinoids (CBD, THC), 2-APB, and osmotic or chemical stress. It contributes to processes including cardiomyocyte function, immune cell activation (phagocytosis in macrophages), neurite outgrowth, and cancer progression. - TRPV3 is heavily expressed in skin, but also found in brain and other organs. It senses warm temperatures (31–39 °C) and is activated by a variety of physical and chemical stimuli including 2-APB, camphor, and carvacrol. TRPV3 is critical for temperature sensation, pain perception, skin barrier formation, wound healing, hair growth, inflammation, itching, and certain skin diseases (e.g., Olmsted syndrome). Both channels are emerging drug targets, with modulators under investigation for treating cardiovascular disease, cancer, inflammatory conditions, pruritus, and skin disorders. Structural differences between TRPV2 and TRPV3 determine their unique gating mechanisms and pharmacological sensitivities.

Other names

TRPV2: Vanilloid receptor-like protein 1, VRL-1TRPV3: Osm-9-like TRP channel 3, VR-OAC, VRL3

Modulators act as agonists or antagonists to alter channel gating, primarily leading to opening (agonism) or blocking (antagonism/inhibition) of the calcium-permeable pore.