Tclin TRPV1 Transient receptor potential cation channel subfamily V member 1

Protein Summary

Description

Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis. Capsaicin, the main pungent ingredient in hot chili peppers, elicits a sensation of burning pain by selectively activating sensory neurons that convey information about noxious stimuli to the central nervous system. The protein encoded by this gene is a receptor for capsaicin and is a non-selective cation channel that is structurally related to members of the TRP family of ion channels. This receptor is also activated by increases in temperature in the noxious range, suggesting that it functions as a transducer of painful thermal stimuli in vivo. Four transcript variants encoding the same protein, but with different 5' UTR sequence, have been described for this gene. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q8NER1
• A2RUA9
• Q3LU47
• Q9H0G9
• Q9H303
• Q9H304
• Q9NQ74
• Q9NY22
• TrpV1

Gene Name

• TRPV1

Ensembl ID

• ENST00000399756
• ENSP00000382659
• ENSG00000196689
• ENST00000399759
• ENSP00000382661
• ENST00000571088
• ENSP00000461007
• ENST00000572705
• ENSP00000459962

Symbol

• VR1
• VR1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
chemical	1
molecular function	1
ligand (chemical)	0.97
biological term	0.94
cellular component	0.8

Protein Classes

PANTHER Classes

Protein / Transporter / Ion Channel / Transient Receptor Potential Cation Channel Subfamily V Member 1

DTO Classes

Protein / Ion Channel / Transient Receptor Potential Calcium Channel (Trp-cc) Family / Trpv Subfamily / Trpv1 Sub-subfamily / Transient Receptor Potential Cation Channel Subfamily V Member 1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 6643.12   (req: < 5)

Gene RIFs: 427   (req: <= 3)

Antibodies: 493   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 6643.12   (req: >= 5)

Gene RIFs: 427   (req: > 3)

Antibodies: 493   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 49

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 3290

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 4