Target intelligence / Profile preview

Transient receptor potential vanilloid 2 channel (TRPV2)

Target
TRPV2
Molecular classification
Ion channel, Transient receptor potential (TRP) channel, Cation channel, Receptor
01

Overview

The **Transient receptor potential vanilloid 2 channel (TRPV2)** is a member of the TRP superfamily of cation channels, widely recognized as a non-selective, calcium-permeable ion channel within the vanilloid subfamily[1][3]. While homologous to TRPV1, TRPV2 has distinct activation properties and is insensitive to classic TRPV1 agonists like capsaicin and heat[1][4]. TRPV2 plays roles in signal transduction associated with mechanosensation, nociception, and osmotic regulation, and is expressed in a range of tissues including sensory neurons, immune cells, and the heart[5][6]. Structurally, TRPV2 forms a tetrameric channel with conserved pore domains and ankyrin repeat domains facilitating protein-protein interactions and gating regulation[6]. TRPV2 has been implicated in cancer, inflammation, and neurological and cardiovascular disorders, making it an emerging therapeutic target with modulators such as cannabidiol and 2-APB being active at the channel[7][8][3]. Safety considerations for drugs targeting TRPV2 include potential disruptions to cellular calcium handling and off-target effects due to homology with other TRPV family members.

Other names
Transient receptor potential cation channel subfamily V member 2TRPV2 channelOsm-9-like TRP channel 2
02

Mechanism of action

Agonists and modulators can activate or inhibit channel opening, altering cation flow (primarily Ca²⁺ and Na²⁺), leading to changes in cell signaling and excitability

03

Biological functions

Signal transductionNociceptionMechanosensationOsmoregulationCation transportCell proliferation
04

Disease associations

CancerInflammationNeurological disordersImmunological disordersCardiovascular disease
05

Safety considerations

Potential adverse effects due to altered calcium homeostasisunknown selectivity in vivo for channel modulatorspotential off-target effects in tissues expressing multiple TRP channels
06

Interacting drugs

Cannabidiol (CBD)

4 more in the full profile.

07

Biomarkers

Currently no widely established biomarkers for patient selection; research ongoing regarding TRPV2 expression as a prognostic factor in certain cancers

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