Target Information

Target General Infomation
Target ID
T58496
Former ID
TTDR01258
Target Name
Transient receptor potential cation channel subfamily V member 3
Gene Name
TRPV3
Synonyms
TrpV3; VRL-3; Vanilloid receptor-like 3; TRPV3
Target Type
Clinical Trial
Disease Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Function
Putative receptor-activated non-selective calcium permeant cation channel. It is activated by innocuous (warm) temperatures and shows an increased response at noxious temperatures greater than 39 degrees Celsius. Activation exhibits an outward rectification. May associate with TRPV1 and may modulate its activity. Is a negative regulator of hair growth and cycling: TRPV3-coupled signaling suppresses keratinocyte proliferation in hair follicles and induces apoptosis and premature hair follicle regression (catagen).
BioChemical Class
Transient receptor potential catioin channel
UniProt ID
Q8NET8
Sequence
MKAHPKEMVPLMGKRVAAPSGNPAILPEKRPAEITPTKKSAHFFLEIEGFEPNPTVAKTS
PPVFSKPMDSNIRQCISGNCDDMDSPQSPQDDVTETPSNPNSPSAQLAKEEQRRKKRRLK
KRIFAAVSEGCVEELVELLVELQELCRRRHDEDVPDFLMHKLTASDTGKTCLMKALLNIN
PNTKEIVRILLAFAEENDILGRFINAEYTEEAYEGQTALNIAIERRQGDIAALLIAAGAD
VNAHAKGAFFNPKYQHEGFYFGETPLALAACTNQPEIVQLLMEHEQTDITSRDSRGNNIL
HALVTVAEDFKTQNDFVKRMYDMILLRSGNWELETTRNNDGLTPLQLAAKMGKAEILKYI
LSREIKEKRLRSLSRKFTDWAYGPVSSSLYDLTNVDTTTDNSVLEITVYNTNIDNRHEML
TLEPLHTLLHMKWKKFAKHMFFLSFCFYFFYNITLTLVSYYRPREEEAIPHPLALTHKMG
WLQLLGRMFVLIWAMCISVKEGIAIFLLRPSDLQSILSDAWFHFVFFIQAVLVILSVFLY
LFAYKEYLACLVLAMALGWANMLYYTRGFQSMGMYSVMIQKVILHDVLKFLFVYIVFLLG
FGVALASLIEKCPKDNKDCSSYGSFSDAVLELFKLTIGLGDLNIQQNSKYPILFLFLLIT
YVILTFVLLLNMLIALMGETVENVSKESERIWRLQRARTILEFEKMLPEWLRSRFRMGEL
CKVAEDDFRLCLRINEVKWTEWKTHVSFLNEDPGPVRRTDFNKIQDSSRNNSKTTLNAFE
EVEEFPETSV
Drugs and Mode of Action
Drug(s) SAR292833 Drug Info Phase 2 Pain [532424]
Activator 2-APB Drug Info [527098]
6-tert-butyl-m-cresol Drug Info [528784]
borneol Drug Info [528784]
carvacrol Drug Info [528138]
carveol Drug Info [528784]
cinnamaldehyde Drug Info [528302]
citral Drug Info [529456]
dihydrocarveol Drug Info [528784]
diphenylboronic anhydride Drug Info [527445]
incensole acetate Drug Info [529482]
tetrahydrocannabivarin Drug Info [531540]
Blocker (channel blocker) aspirin-triggered resolvin D1 Drug Info [531538]
diphenyltetrahydrofuran Drug Info [527445]
Agonist EDP-18 Drug Info [543862]
Modulator SAR292833 Drug Info [532424]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Inflammatory mediator regulation of TRP channels
Reactome TRP channels
References
Ref 532424Pharmacological profiling of the TRPV3 channel in recombinant and native assays. Br J Pharmacol. 2014 May;171(10):2631-44.
Ref 5270982-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J Neurosci. 2004 Jun 2;24(22):5177-82.
Ref 527445Biphasic currents evoked by chemical or thermal activation of the heat-gated ion channel, TRPV3. J Biol Chem. 2005 Apr 22;280(16):15928-41. Epub 2005 Feb 18.
Ref 528138Oregano, thyme and clove-derived flavors and skin sensitizers activate specific TRP channels. Nat Neurosci. 2006 May;9(5):628-35. Epub 2006 Apr 16.
Ref 528302More than cool: promiscuous relationships of menthol and other sensory compounds. Mol Cell Neurosci. 2006 Aug;32(4):335-43. Epub 2006 Jul 7.
Ref 528784Monoterpenoid agonists of TRPV3. Br J Pharmacol. 2007 Jun;151(4):530-40. Epub 2007 Apr 10.
Ref 529456Citral sensing by Transient [corrected] receptor potential channels in dorsal root ganglion neurons. PLoS One. 2008 May 7;3(5):e2082.
Ref 529482Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain. FASEB J. 2008 Aug;22(8):3024-34.
Ref 53153817(R)-resolvin D1 specifically inhibits transient receptor potential ion channel vanilloid 3 leading to peripheral antinociception. Br J Pharmacol. 2012 Feb;165(3):683-92.
Ref 531540Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation. Acta Physiol (Oxf). 2012 Feb;204(2):255-66.
Ref 532424Pharmacological profiling of the TRPV3 channel in recombinant and native assays. Br J Pharmacol. 2014 May;171(10):2631-44.
Ref 543862(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 509).

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