Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T58496
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| Former ID |
TTDR01258
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| Target Name |
Transient receptor potential cation channel subfamily V member 3
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| Gene Name |
TRPV3
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| Synonyms |
TrpV3; VRL-3; Vanilloid receptor-like 3; TRPV3
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| Target Type |
Clinical Trial
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| 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).
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| BioChemical Class |
Transient receptor potential catioin channel
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| UniProt ID | |||||
| Sequence |
MKAHPKEMVPLMGKRVAAPSGNPAILPEKRPAEITPTKKSAHFFLEIEGFEPNPTVAKTS
PPVFSKPMDSNIRQCISGNCDDMDSPQSPQDDVTETPSNPNSPSAQLAKEEQRRKKRRLK KRIFAAVSEGCVEELVELLVELQELCRRRHDEDVPDFLMHKLTASDTGKTCLMKALLNIN PNTKEIVRILLAFAEENDILGRFINAEYTEEAYEGQTALNIAIERRQGDIAALLIAAGAD VNAHAKGAFFNPKYQHEGFYFGETPLALAACTNQPEIVQLLMEHEQTDITSRDSRGNNIL HALVTVAEDFKTQNDFVKRMYDMILLRSGNWELETTRNNDGLTPLQLAAKMGKAEILKYI LSREIKEKRLRSLSRKFTDWAYGPVSSSLYDLTNVDTTTDNSVLEITVYNTNIDNRHEML TLEPLHTLLHMKWKKFAKHMFFLSFCFYFFYNITLTLVSYYRPREEEAIPHPLALTHKMG WLQLLGRMFVLIWAMCISVKEGIAIFLLRPSDLQSILSDAWFHFVFFIQAVLVILSVFLY LFAYKEYLACLVLAMALGWANMLYYTRGFQSMGMYSVMIQKVILHDVLKFLFVYIVFLLG FGVALASLIEKCPKDNKDCSSYGSFSDAVLELFKLTIGLGDLNIQQNSKYPILFLFLLIT YVILTFVLLLNMLIALMGETVENVSKESERIWRLQRARTILEFEKMLPEWLRSRFRMGEL CKVAEDDFRLCLRINEVKWTEWKTHVSFLNEDPGPVRRTDFNKIQDSSRNNSKTTLNAFE EVEEFPETSV |
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| Drugs and Mode of Action | |||||
| Drug(s) | SAR292833 | Drug Info | Phase 2 | Pain | [1] |
| Activator | 2-APB | Drug Info | [2] | ||
| 6-tert-butyl-m-cresol | Drug Info | [3] | |||
| borneol | Drug Info | [3] | |||
| carvacrol | Drug Info | [4] | |||
| carveol | Drug Info | [3] | |||
| cinnamaldehyde | Drug Info | [5] | |||
| citral | Drug Info | [6] | |||
| dihydrocarveol | Drug Info | [3] | |||
| diphenylboronic anhydride | Drug Info | [7] | |||
| incensole acetate | Drug Info | [8] | |||
| tetrahydrocannabivarin | Drug Info | [9] | |||
| Blocker (channel blocker) | aspirin-triggered resolvin D1 | Drug Info | [10] | ||
| diphenyltetrahydrofuran | Drug Info | [7] | |||
| Agonist | EDP-18 | Drug Info | [11] | ||
| Modulator | SAR292833 | Drug Info | [1] | ||
| 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 1 | Pharmacological profiling of the TRPV3 channel in recombinant and native assays. Br J Pharmacol. 2014 May;171(10):2631-44. | ||||
| REF 2 | 2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J Neurosci. 2004 Jun 2;24(22):5177-82. | ||||
| REF 3 | Monoterpenoid agonists of TRPV3. Br J Pharmacol. 2007 Jun;151(4):530-40. Epub 2007 Apr 10. | ||||
| REF 4 | Oregano, 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 5 | More than cool: promiscuous relationships of menthol and other sensory compounds. Mol Cell Neurosci. 2006 Aug;32(4):335-43. Epub 2006 Jul 7. | ||||
| REF 6 | Citral sensing by Transient [corrected] receptor potential channels in dorsal root ganglion neurons. PLoS One. 2008 May 7;3(5):e2082. | ||||
| REF 7 | Biphasic 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 8 | Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain. FASEB J. 2008 Aug;22(8):3024-34. | ||||
| REF 9 | Cannabinoid 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 10 | 17(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 11 | (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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