TRPV2 | Transient Receptor Potential Cation Channel Subfamily V Member 2

TRPV2 is a Calcium-permeable, non-selective cation channel with an outward rectification. Among the TRPV subfamily, TRPV2 and TRPV1 share 50% of their sequence identity. However, TRPV2 is not activated by capsaicin (which is an activator of TRPV1) nor by an acidic pH. TRPV2 can open in response to a variety of stimuli including hormones, growth factors, mechanical stretching, heat (greater than 52°C), osmotic swelling, lysophospholipids, and cannabinoids.

Gene:
TRPV2

Human Protein:
UniProt Q9Y5S1

Tissue:
Motor neurons, large sensory neurons, brain, MIN6 cells (β-cell type), spinal cord, heart, lymph nodes, spleen, appendix, placenta with highest expression levels in the lungs

Function/ Application:
In immune cells, TRPV2 mediates cytokine release, phagocytosis, endocytosis, podosome assembly, and inflammation. It is suggested that TRPV2 may act as a mechanosensor in circulatory organs. TRPV2 plays a role in negative homeostatic control of excess cell proliferation by inducing apoptosis . Activation of TRPV2 by growth factors and hormones induces the receptor to translocate from intracellular compartments to the plasma membrane, which initiates the development of death signals. The expression of TRPV2 in MIN6 cells suggest a role in glucose homeostasis. TRPV2 has been shown to be involved in stretch-dependent responses in heart cells. TRPV1 translocates to cell surface in response to IGF-1 to induce a constitutively active conductance. As well, it translocates to the cell surface in response to membrane stretch.

Pathology:
Retina lymphoma, Dentin sensitivity
Cancer: The over-expression of TRPV2 has been linked to several cancer types. In gliomas, TRPV2 expression leads to resistance to apoptotic cell death, leading to harmful, carcinogenic cell survival.
Epilepsy: The cannabis constituent, cannabidiol (CBD), is a compound that acts in the release of neurotransmitters in the brain and has been researched for its positive effects in the treatment of epilepsy. CBD is able to bind to TRPV2 which results in a reduction of epileptic activity.

Interaction:
PRKAR2A, PRKAR2B, ACBD3, SLC50A1, TRPV1

Modulator:
Cannabidiol, Amiloride, Probenecid, 2-APB, La³⁺, amiloride, ruthenium red, fampridine

Assays:
Patch Clamp: whole cell

Recommended Reviews:
International Union of Pharmacology. XLIII. Compendium of voltage-gated ion channels: transient receptor potential channels., Pharmacol Rev 55(4):591-6 Clapham, et al. 2003