Biology:TRPV3

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Short description: Protein-coding gene in the species Homo sapiens


A representation of the 3D structure of the protein myoglobin showing turquoise α-helices.
Generic protein structure example

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.[1]

Function

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.[2] Mice lacking these protein are unable to sense elevated temperatures (>33 °C) but are able to sense cold and noxious heat.[3] 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.[4] The role of TRPV3 channels in the brain is unclear, but appears to play a role in mood regulation.[5] The protective effects of the natural product, incensole acetate were partially mediated by TRPV3 channels.[6]

Modulation

The TRPV3 channel is directly activated by various natural compounds like carvacrol, thymol and eugenol.[7] Several other monoterpenoids which cause either feeling of warmth or are skin sensitizers can also open the channel.[8] Monoterpenoids also induce agonist-specific desensitization of TRPV3 channels in a calcium-independent manner.[9]

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.[10][11][12][13][14]

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.[15] Drofenine also acts as a TRPV3 agonist in addition to its other actions.[16] Conversely, icilin has been shown to act as a TRPV3 antagonist, as well as a TRPM8 agonist.[17] Forsythoside B acts as a TRPV3 inhibitor among other actions.[18] Farnesyl pyrophosphate is an endogenous agonist of TRPV3,[19] while incensole acetate from frankincense also acts as an agonist at TRPV3.[20] TRPV3-74a is a selective TRPV3 antagonist.[21]

Ligands

Agonists

See also

References

  1. ↑ "Entrez Gene: TRPV3 transient receptor potential cation channel, subfamily V, member 3". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=162514. 
  2. ↑ "A heat-sensitive TRP channel expressed in keratinocytes". Science 296 (5575): 2046–9. June 2002. doi:10.1126/science.1073140. PMID 12016205. Bibcode: 2002Sci...296.2046P. 
  3. ↑ "Impaired thermosensation in mice lacking TRPV3, a heat and camphor sensor in the skin". Science 307 (5714): 1468–72. March 2005. doi:10.1126/science.1108609. PMID 15746429. Bibcode: 2005Sci...307.1468M. 
  4. ↑ "Influence of TRPV3 mutation on hair growth cycle in mice". Biochemical and Biophysical Research Communications 363 (3): 479–83. November 2007. doi:10.1016/j.bbrc.2007.08.170. PMID 17888882. 
  5. ↑ "Incense on the brain, by Ran Shapira, Haaretz". Haaretz. http://www.haaretz.com/print-edition/features/incense-on-the-brain-1.248292. 
  6. ↑ "Protective effects of incensole acetate on cerebral ischemic injury". Brain Research 1443: 89–97. March 2012. doi:10.1016/j.brainres.2012.01.001. PMID 22284622. 
  7. ↑ "Oregano, thyme and clove-derived flavors and skin sensitizers activate specific TRP channels". Nat. Neurosci. 9 (5): 628–35. 2006. doi:10.1038/nn1692. PMID 16617338. 
  8. ↑ "Monoterpenoid agonists of TRPV3". Br. J. Pharmacol. 151 (4): 530–40. 2007. doi:10.1038/sj.bjp.0707245. PMID 17420775. 
  9. ↑ "Monoterpenoids Induce Agonist-Specific Desensitization of Transient Receptor Potential Vanilloid-3 (TRPV3) ion Channels". J Pharm Pharm Sci 12 (1): 116–128. 2009. doi:10.18433/j37c7k. PMID 19470296. 
  10. ↑ "Roles of resolvins in the resolution of acute inflammation". Cell Biology International 39 (1): 3–22. 2015. doi:10.1002/cbin.10345. PMID 25052386. 
  11. ↑ "Lipid mediators in the resolution of inflammation". Cold Spring Harbor Perspectives in Biology 7 (2): a016311. 2015. doi:10.1101/cshperspect.a016311. PMID 25359497. 
  12. ↑ "Biological Roles of Resolvins and Related Substances in the Resolution of Pain". BioMed Research International 2015: 830930. 2015. doi:10.1155/2015/830930. PMID 26339646. 
  13. ↑ "Emerging roles of resolvins in the resolution of inflammation and pain". Trends in Neurosciences 34 (11): 599–609. 2011. doi:10.1016/j.tins.2011.08.005. PMID 21963090. 
  14. ↑ "The resolution code of acute inflammation: Novel pro-resolving lipid mediators in resolution". Seminars in Immunology 27 (3): 200–15. 2015. doi:10.1016/j.smim.2015.03.004. PMID 25857211. 
  15. ↑ "2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3". The Journal of Neuroscience 24 (22): 5177–82. June 2004. doi:10.1523/JNEUROSCI.0934-04.2004. PMID 15175387. 
  16. ↑ "Drofenine: A 2-APB Analogue with Greater Selectivity for Human TRPV3". Pharmacology Research & Perspectives 2 (5): e00062. October 2014. doi:10.1002/prp2.62. PMID 25089200. 
  17. ↑ "Supercooling agent icilin blocks a warmth-sensing ion channel TRPV3". TheScientificWorldJournal 2012: 982725. 2012. doi:10.1100/2012/982725. PMID 22548000. 
  18. ↑ "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. January 2019. doi:10.1124/jpet.118.254045. PMID 30377214. 
  19. ↑ "Farnesyl pyrophosphate is a novel pain-producing molecule via specific activation of TRPV3". The Journal of Biological Chemistry 285 (25): 19362–71. June 2010. doi:10.1074/jbc.M109.087742. PMID 20395302. 
  20. ↑ "Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain". FASEB Journal 22 (8): 3024–34. August 2008. doi:10.1096/fj.07-101865. PMID 18492727. 
  21. ↑ "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. May 2016. doi:10.1021/acs.jmedchem.6b00287. PMID 27077528. 

Further reading

  • Islam, Md. Shahidul (January 2011). Transient Receptor Potential Channels. Advances in Experimental Medicine and Biology. 704. Berlin: Springer. pp. 700. ISBN 978-94-007-0264-6. 
  • "International Union of Pharmacology. XLIX. Nomenclature and structure-function relationships of transient receptor potential channels.". Pharmacol. Rev. 57 (4): 427–50. 2006. doi:10.1124/pr.57.4.6. PMID 16382100. 

External links

This article incorporates text from the United States National Library of Medicine, which is in the public domain.



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