TRPV3

TRPV3
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesTRPV3, FNEPPK2, OLMS, VRL3, transient receptor potential cation channel subfamily V member 3, OLMS1
External IDsOMIM: 607066; MGI: 2181407; HomoloGene: 17040; GeneCards: TRPV3; OMA:TRPV3 - orthologs
Orthologs
SpeciesHumanMouse
Entrez

162514

246788

Ensembl

ENSG00000167723

ENSMUSG00000043029

UniProt

Q8NET8

Q8K424

RefSeq (mRNA)

NM_001258205
NM_145068

NM_145099
NM_001371006

RefSeq (protein)

NP_001245134
NP_659505

NP_659567
NP_001357935

Location (UCSC)Chr 17: 3.51 – 3.56 MbChr 11: 73.16 – 73.19 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Transient receptor potential cation channel, subfamily V, member 3, also known as TRPV3, is a human gene encoding the protein of the same name.

The TRPV3 protein belongs to a family of nonselective cation channels that function in a variety of processes, including temperature sensation and vasoregulation. The thermosensitive members of this family are expressed in subsets of human sensory neurons that terminate in the skin, and are activated at distinct physiological temperatures. This channel is activated at temperatures between 22 and 40 degrees C. The gene lies in close proximity to another family member (TRPV1) gene on chromosome 17, and the two encoded proteins are thought to associate with each other to form heteromeric channels.[5]

Function

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The TRPV3 channel has wide tissue expression that is especially high in the skin (keratinocytes) but also in the brain. It functions as a molecular sensor for innocuous warm temperatures.[6] Mice lacking these protein are unable to sense elevated temperatures (>33 °C) but are able to sense cold and noxious heat.[7] In addition to thermosensation TRPV3 channels seem to play a role in hair growth because mutations in the TRPV3 gene cause hair loss in mice.[8] The role of TRPV3 channels in the brain is unclear, but appears to play a role in mood regulation.[9] The protective effects of the natural product, incensole acetate were partially mediated by TRPV3 channels.[10]

Modulation

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The TRPV3 channel is directly activated by various natural compounds like carvacrol, thymol and eugenol.[11] Several other monoterpenoids which cause either feeling of warmth or are skin sensitizers can also open the channel.[12] Monoterpenoids also induce agonist-specific desensitization of TRPV3 channels in a calcium-independent manner.[13]

Resolvin E1 (RvE1), RvD2, and 17R-RvD1 (see resolvins) are metabolites of the omega 3 fatty acids, eicosapentaenoic acid (for RvE1) or docosahexaenoic acid (for RvD2 and 17R-RvD1). These metabolites are members of the specialized proresolving mediators (SPMs) class of metabolites that function to resolve diverse inflammatory reactions and diseases in animal models and, it is proposed, humans. These SPMs also dampen pain perception arising from various inflammation-based causes in animal models. The mechanism behind their pain-dampening effects involves the inhibition of TRPV3, probably (in at least certain cases) by an indirect effect wherein they activate other receptors located on neurons or nearby microglia or astrocytes. CMKLR1, GPR32, FPR2, and NMDA receptors have been proposed to be the receptors through which these SPMs operate to down-regulate TRPV3 and thereby pain perception.[14][15][16][17][18]

2-Aminoethoxydiphenyl borate (2-APB) is a mixed agonist-antagonist of the TRPV3 receptor, acting as an antagonist at low concentrations but showing agonist activity when used in larger amounts.[19] Drofenine also acts as a TRPV3 agonist in addition to its other actions.[20] Conversely, icilin has been shown to act as a TRPV3 antagonist, as well as a TRPM8 agonist.[21] Forsythoside B acts as a TRPV3 inhibitor among other actions.[22] Farnesyl pyrophosphate is an endogenous agonist of TRPV3,[23] while incensole acetate from frankincense also acts as an agonist at TRPV3.[24] TRPV3-74a is a selective TRPV3 antagonist.[25]

Ligands

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Agonists

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See also

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References

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  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000167723 – Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000043029 – Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ "Entrez Gene: TRPV3 transient receptor potential cation channel, subfamily V, member 3".
  6. ^ Peier AM, Reeve AJ, Andersson DA, Moqrich A, Earley TJ, Hergarden AC, et al. (June 2002). "A heat-sensitive TRP channel expressed in keratinocytes". Science. 296 (5575): 2046–9. Bibcode:2002Sci...296.2046P. doi:10.1126/science.1073140. PMID 12016205. S2CID 6180133.
  7. ^ Moqrich A, Hwang SW, Earley TJ, Petrus MJ, Murray AN, Spencer KS, et al. (March 2005). "Impaired thermosensation in mice lacking TRPV3, a heat and camphor sensor in the skin". Science. 307 (5714): 1468–72. Bibcode:2005Sci...307.1468M. doi:10.1126/science.1108609. PMID 15746429. S2CID 11504772.
  8. ^ Imura K, Yoshioka T, Hikita I, Tsukahara K, Hirasawa T, Higashino K, et al. (November 2007). "Influence of TRPV3 mutation on hair growth cycle in mice". Biochemical and Biophysical Research Communications. 363 (3): 479–83. doi:10.1016/j.bbrc.2007.08.170. PMID 17888882.
  9. ^ "Incense on the brain, by Ran Shapira, Haaretz". Haaretz.
  10. ^ Moussaieff A, Yu J, Zhu H, Gattoni-Celli S, Shohami E, Kindy MS (March 2012). "Protective effects of incensole acetate on cerebral ischemic injury". Brain Research. 1443: 89–97. doi:10.1016/j.brainres.2012.01.001. PMC 3294134. PMID 22284622.
  11. ^ Xu H, Delling M, Jun JC, Clapham DE (2006). "Oregano, thyme and clove-derived flavors and skin sensitizers activate specific TRP channels". Nat. Neurosci. 9 (5): 628–35. doi:10.1038/nn1692. PMID 16617338. S2CID 13088422.
  12. ^ Vogt-Eisele AK, Weber K, Sherkheli MA, et al. (2007). "Monoterpenoid agonists of TRPV3". Br. J. Pharmacol. 151 (4): 530–40. doi:10.1038/sj.bjp.0707245. PMC 2013969. PMID 17420775.
  13. ^ Sherkheli MA, et al. (2009). "Monoterpenoids Induce Agonist-Specific Desensitization of Transient Receptor Potential Vanilloid-3 (TRPV3) ion Channels". J Pharm Pharm Sci. 12 (1): 116–128. doi:10.18433/j37c7k. PMID 19470296.
  14. ^ Qu Q, Xuan W, Fan GH (2015). "Roles of resolvins in the resolution of acute inflammation". Cell Biology International. 39 (1): 3–22. doi:10.1002/cbin.10345. PMID 25052386. S2CID 10160642.
  15. ^ Serhan CN, Chiang N, Dalli J, Levy BD (2015). "Lipid mediators in the resolution of inflammation". Cold Spring Harbor Perspectives in Biology. 7 (2): a016311. doi:10.1101/cshperspect.a016311. PMC 4315926. PMID 25359497.
  16. ^ Lim JY, Park CK, Hwang SW (2015). "Biological Roles of Resolvins and Related Substances in the Resolution of Pain". BioMed Research International. 2015: 830930. doi:10.1155/2015/830930. PMC 4538417. PMID 26339646.
  17. ^ Ji RR, Xu ZZ, Strichartz G, Serhan CN (2011). "Emerging roles of resolvins in the resolution of inflammation and pain". Trends in Neurosciences. 34 (11): 599–609. doi:10.1016/j.tins.2011.08.005. PMC 3200462. PMID 21963090.
  18. ^ Serhan CN, Chiang N, Dalli J (2015). "The resolution code of acute inflammation: Novel pro-resolving lipid mediators in resolution". Seminars in Immunology. 27 (3): 200–15. doi:10.1016/j.smim.2015.03.004. PMC 4515371. PMID 25857211.
  19. ^ Chung MK, Lee H, Mizuno A, Suzuki M, Caterina MJ (June 2004). "2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3". The Journal of Neuroscience. 24 (22): 5177–82. doi:10.1523/JNEUROSCI.0934-04.2004. PMC 6729202. PMID 15175387.
  20. ^ Deering-Rice CE, Mitchell VK, Romero EG, Abdel Aziz MH, Ryskamp DA, Križaj D, et al. (October 2014). "Drofenine: A 2-APB Analogue with Greater Selectivity for Human TRPV3". Pharmacology Research & Perspectives. 2 (5): e00062. doi:10.1002/prp2.62. PMC 4115637. PMID 25089200.
  21. ^ Sherkheli MA, Gisselmann G, Hatt H (2012). "Supercooling agent icilin blocks a warmth-sensing ion channel TRPV3". TheScientificWorldJournal. 2012: 982725. doi:10.1100/2012/982725. PMC 3324214. PMID 22548000.
  22. ^ Zhang H, Sun X, Qi H, Ma Q, Zhou Q, Wang W, Wang K (January 2019). "Pharmacological Inhibition of the Temperature-Sensitive and Ca2+-Permeable Transient Receptor Potential Vanilloid TRPV3 Channel by Natural Forsythoside B Attenuates Pruritus and Cytotoxicity of Keratinocytes". The Journal of Pharmacology and Experimental Therapeutics. 368 (1): 21–31. doi:10.1124/jpet.118.254045. PMID 30377214.
  23. ^ Bang S, Yoo S, Yang TJ, Cho H, Hwang SW (June 2010). "Farnesyl pyrophosphate is a novel pain-producing molecule via specific activation of TRPV3". The Journal of Biological Chemistry. 285 (25): 19362–71. doi:10.1074/jbc.M109.087742. PMC 2885216. PMID 20395302.
  24. ^ Moussaieff A, Rimmerman N, Bregman T, Straiker A, Felder CC, Shoham S, et al. (August 2008). "Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain". FASEB Journal. 22 (8): 3024–34. doi:10.1096/fj.07-101865. PMC 2493463. PMID 18492727.
  25. ^ Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, et al. (May 2016). "Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists". Journal of Medicinal Chemistry. 59 (10): 4926–47. doi:10.1021/acs.jmedchem.6b00287. PMID 27077528.

Further reading

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  • Islam MS (January 2011). Transient Receptor Potential Channels. Advances in Experimental Medicine and Biology. Vol. 704. Berlin: Springer. p. 700. ISBN 978-94-007-0264-6.
  • Clapham DE, Julius D, Montell C, Schultz G (2006). "International Union of Pharmacology. XLIX. Nomenclature and structure-function relationships of transient receptor potential channels". Pharmacol. Rev. 57 (4): 427–50. doi:10.1124/pr.57.4.6. PMID 16382100. S2CID 17936350.
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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