GPR55
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G protein-coupled receptor 55
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| Identifiers | ||||||||||||||
| Symbol(s) | GPR55; | |||||||||||||
| External IDs | OMIM: 604107 MGI: 2685064 HomoloGene: 36184 | |||||||||||||
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| Orthologs | ||||||||||||||
| Human | Mouse | |||||||||||||
| Entrez | 9290 | 227326 | ||||||||||||
| Ensembl | ENSG00000135898 | ENSMUSG00000049608 | ||||||||||||
| Uniprot | Q9Y2T6 | Q14BV9 | ||||||||||||
| Refseq | NM_005683 (mRNA) NP_005674 (protein) |
NM_001033290 (mRNA) NP_001028462 (protein) |
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| Location | Chr 2: 231.48 - 231.5 Mb | Chr 1: 87.77 - 87.79 Mb | ||||||||||||
| Pubmed search | [1] | [2] | ||||||||||||
G protein-coupled receptor 55, also known as GPR55, is a human gene which encodes the protein for the GPR-55 receptor.[1]
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[edit] History
GPR55 was identified and cloned for the first time in 1999.[2] Later it was identified by an in silico screen as a putative cannabinoid receptor because of a similar amino acid sequence in the binding region.[3] Research groups from Glaxo Smith Kline and Astra Zeneca characterized the receptor extensively because it was hoped to be responsible for the blood pressure lowering properties of cannabinoids. GPR55 is indeed activated by endogenous, plant and synthetic cannabinoids but GPR-55 knockout mice generated by a research group from Glaxo Smith Kline showed no altered blood pressure regulation after administration of the cannabidiol-derivative abnormal cannabidiol.[4]
[edit] Signal cascade
GPR55 is coupled to the G-protein G13 and activation of the receptor leads to stimulation of rhoA, cdc42 and rac1.[5]
[edit] Pharmacology
GPR55 is activated by the plant cannabinoids Δ9-THC and cannabidiol,[6] and the endocannabinoids anandamide, 2-AG, noladin ether in the low nanomolar range. The synthetic cannabinoid CP-55940 is also able to activate the receptor[6] while the structurally unrelated cannabinoid mimic WIN 55,212-2 fails to activate the receptor.[4]
[edit] Physiological function
The physiological role of GPR55 is unclear. Mice with a target deletion of the GPR55 gene show no specific phenotype.[4] GPR55 is widely expressed in the brain, especially in the cerebellum. Except for the jejunum and ileum it is not expressed in the periphery.[6]
[edit] References
- ^ Entrez Gene: GPR55 G protein-coupled receptor 55.
- ^ Sawzdargo M, Nguyen T, Lee DK, Lynch KR, Cheng R, Heng HH, George SR, O'Dowd BF (1999). "Identification and cloning of three novel human G protein-coupled receptor genes GPR52, PsiGPR53 and GPR55: GPR55 is extensively expressed in human brain". Brain Res. Mol. Brain Res. 64 (2): 193–8. doi:. PMID 9931487.
- ^ Baker D, Pryce G, Davies WL, Hiley CR (2006). "In silico patent searching reveals a new cannabinoid receptor". Trends Pharmacol. Sci. 27 (1): 1–4. doi:. PMID 16318877.
- ^ a b c Johns DG, Behm DJ, Walker DJ, Ao Z, Shapland EM, Daniels DA, Riddick M, Dowell S, Staton PC, Green P, Shabon U, Bao W, Aiyar N, Yue TL, Brown AJ, Morrison AD, Douglas SA (2007). "The novel endocannabinoid receptor GPR55 is activated by atypical cannabinoids but does not mediate their vasodilator effects". Br. J. Pharmacol. 152 (5): 825–31. doi:. PMID 17704827.
- ^ Lauckner JE, Jensen JB, Chen HY, Lu HC, Hille B, Mackie K (2008). "GPR55 is a cannabinoid receptor that increases intracellular calcium and inhibits M current". Proc. Natl. Acad. Sci. U.S.A. 105 (7): 2699–704. doi:. PMID 18263732.
- ^ a b c Ryberg E, Larsson N, Sjögren S, Hjorth S, Hermansson NO, Leonova J, Elebring T, Nilsson K, Drmota T, Greasley PJ (2007). "The orphan receptor GPR55 is a novel cannabinoid receptor". Br. J. Pharmacol. 152 (7): 1092–101. doi:. PMID 17876302.
[edit] Further reading
- Sawzdargo M, Nguyen T, Lee DK, et al. (1999). "Identification and cloning of three novel human G protein-coupled receptor genes GPR52, PsiGPR53 and GPR55: GPR55 is extensively expressed in human brain.". Brain Res. Mol. Brain Res. 64 (2): 193–8. PMID 9931487.
- Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:. PMID 12477932.
- Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7. doi:. PMID 15489334.
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