Melatonin receptor 1B
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| Melatonin receptor 1B | |||||||||||||
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| Identifiers | |||||||||||||
| Symbols | MTNR1B; MT2; MEL-1B-R | ||||||||||||
| External IDs | OMIM: 600804 MGI: 2181726 HomoloGene: 4350 IUPHAR: MT2 GeneCards: MTNR1B Gene | ||||||||||||
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| RNA expression pattern | |||||||||||||
| 250px | |||||||||||||
| More reference expression data | |||||||||||||
| Orthologs | |||||||||||||
| Species | Human | Mouse | |||||||||||
| Entrez | 4544 | 244701 | |||||||||||
| Ensembl | ENSG00000134640 | ENSMUSG00000050901 | |||||||||||
| UniProt | P49286 | P70329 | |||||||||||
| RefSeq (mRNA) | NM_005959 | NM_145712 | |||||||||||
| RefSeq (protein) | NP_005950 | NP_663758 | |||||||||||
| Location (UCSC) | Chr 11: 92.34 - 92.36 Mb | Chr 9: 15.61 - 15.62 Mb | |||||||||||
| PubMed search | [1] | [2] | |||||||||||
Melatonin receptor 1B, also known as MTNR1B, is a protein that in humans is encoded by the MTNR1B gene.[1][2]
Contents
Function
This gene encodes the MT2 protein, one of two high-affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. This gene product is an integral membrane protein that is a G-protein coupled, 7-transmembrane receptor. It is found primarily in the retina and brain; however, this detection requires RT-PCR. It is thought to participate in light-dependent functions in the retina and may be involved in the neurobiological effects of melatonin.[1]
Clinical significance
Several studies have identified MTNR1B receptor mutations that are associated with increased average blood sugar level and around a 20 percent elevated risk of developing type 2 diabetes.[3][4][5] MTNR1B mRNA is expressed in human islets, and immunocytochemistry confirms that it is primarily localized in beta cells in islets.[4]
MT2R Ligands
The following MT2R ligands have selectivity over MT1R:
- Compound 3d: antagonist with sub-nM affinity[6]
- Compound 18f: antagonist and compound 18g partial agonist: sub-nM affinity, >100-fold selectivity over MT1[7]
- Compound 14: antagonist[8]
- Compound 13: agonist[9]
See also
References
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<references />, or <references group="..." />External links
- "Melatonin Receptors: MT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Further reading
- Brzezinski A; Brzezinski, Amnon (1997). "Melatonin in humans". N. Engl. J. Med. 336 (3): 186–95. doi:10.1056/NEJM199701163360306. PMID 8988899.
- Reppert SM, Godson C, Mahle CD; et al. (1995). "Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor". Proc. Natl. Acad. Sci. U.S.A. 92 (19): 8734–8. doi:10.1073/pnas.92.19.8734. PMC 41041 Freely accessible. PMID 7568007.
- Reppert SM, Weaver DR, Ebisawa T; et al. (1996). "Cloning of a melatonin-related receptor from human pituitary". FEBS Lett. 386 (2-3): 219–24. doi:10.1016/0014-5793(96)00437-1. PMID 8647286.
- Niles LP, Wang J, Shen L; et al. (2000). "Melatonin receptor mRNA expression in human granulosa cells". Mol. Cell. Endocrinol. 156 (1-2): 107–10. doi:10.1016/S0303-7207(99)00135-5. PMID 10612428.
- Ebisawa T, Uchiyama M, Kajimura N; et al. (2000). "Genetic polymorphisms of human melatonin 1b receptor gene in circadian rhythm sleep disorders and controls". Neurosci. Lett. 280 (1): 29–32. doi:10.1016/S0304-3940(99)00981-7. PMID 10696804.
- Roy D, Angelini NL, Fujieda H; et al. (2001). "Cyclical regulation of GnRH gene expression in GT1-7 GnRH-secreting neurons by melatonin". Endocrinology. 142 (11): 4711–20. doi:10.1210/en.142.11.4711. PMID 11606436.
- Ayoub MA, Couturier C, Lucas-Meunier E; et al. (2002). "Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer". J. Biol. Chem. 277 (24): 21522–8. doi:10.1074/jbc.M200729200. PMID 11940583.
- Yuan L, Collins AR, Dai J; et al. (2003). "MT(1) melatonin receptor overexpression enhances the growth suppressive effect of melatonin in human breast cancer cells". Mol. Cell. Endocrinol. 192 (1-2): 147–56. doi:10.1016/S0303-7207(02)00029-1. PMID 12088876.
- 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:10.1073/pnas.242603899. PMC 139241 Freely accessible. PMID 12477932.
- Slominski A, Pisarchik A, Zbytek B; et al. (2003). "Functional activity of serotoninergic and melatoninergic systems expressed in the skin". J. Cell. Physiol. 196 (1): 144–53. doi:10.1002/jcp.10287. PMID 12767050.
- Ayoub MA, Levoye A, Delagrange P, Jockers R (2004). "Preferential formation of MT1/MT2 melatonin receptor heterodimers with distinct ligand interaction properties compared with MT2 homodimers". Mol. Pharmacol. 66 (2): 312–21. doi:10.1124/mol.104.000398. PMID 15266022.
- 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:10.1101/gr.2596504. PMC 528928 Freely accessible. PMID 15489334.
- Mazna P, Berka K, Jelinkova I; et al. (2005). "Ligand binding to the human MT2 melatonin receptor: the role of residues in transmembrane domains 3, 6, and 7". Biochem. Biophys. Res. Commun. 332 (3): 726–34. doi:10.1016/j.bbrc.2005.05.017. PMID 15913560.
- Ha E, Choe BK, Jung KH; et al. (2005). "Positive relationship between melatonin receptor type 1B polymorphism and rheumatoid factor in rheumatoid arthritis patients in the Korean population". J. Pineal Res. 39 (2): 201–5. doi:10.1111/j.1600-079X.2005.00237.x. PMID 16098099.
- Savaskan E, Jockers R, Ayoub M; et al. (2007). "The MT2 melatonin receptor subtype is present in human retina and decreases in Alzheimer's disease". Current Alzheimer research. 4 (1): 47–51. doi:10.2174/156720507779939823. PMID 17316165.
- Suzuki S, Masui Y, Ohnuki M; et al. (2007). "Induction of metallothionein synthesis by cilostazol in mice and in human cultured neuronal cell lines". Biol. Pharm. Bull. 30 (4): 791–4. doi:10.1248/bpb.30.791. PMID 17409522.
- Qiu XS, Tang NL, Yeung HY; et al. (2007). "Melatonin receptor 1B (MTNR1B) gene polymorphism is associated with the occurrence of adolescent idiopathic scoliosis". Spine. 32 (16): 1748–53. doi:10.1097/BRS.0b013e3180b9f0ff. PMID 17632395.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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- ↑ 1.0 1.1 "Entrez Gene: MTNR1B melatonin receptor 1B".
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ "Gene That Regulates Glucose Levels And Increases Risk For Diabetes Identified". ScienceDaily. 2008-06-28. Retrieved 2009-01-18.; "Body Clock Linked To Diabetes And High Blood Sugar In New Genome-wide Study". ScienceDaily. 2008-12-08. Retrieved 2009-01-18.; "Is There A Relationship Between Sleep-wake Rhythm And Diabetes? A New Gene Variant Influences Fasting Glucose Levels Via The Melatonin Metabolism". ScienceDaily. 2009-01-16. Retrieved 2009-01-18.
- ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.; Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.; Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Staiger H, Machicao F, Schäfer SA; et al. (2008). "Polymorphisms within the novel type 2 diabetes risk locus MTNR1B determine beta-cell function". PLoS ONE. 3 (12): e3962. doi:10.1371/journal.pone.0003962. PMC 2597741 Freely accessible. PMID 19088850.
- ↑ Rivara S, Lodola A, Mor M; et al. (2007). "N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands". J. Med. Chem. 50 (26): 6618–26. doi:10.1021/jm700957j. PMID 18052314.
- ↑ Bedini A, Spadoni G, Gatti G; et al. (2006). "Design and synthesis of N-(3,3-diphenylpropenyl)alkanamides as a novel class of high-affinity MT2-selective melatonin receptor ligands". J. Med. Chem. 49 (25): 7393–403. doi:10.1021/jm060850a. PMID 17149869.
- ↑ Yous S, Durieux-Poissonnier S, Lipka-Belloli E; et al. (2003). "Design and synthesis of 3-phenyl tetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands". Bioorg. Med. Chem. 11 (5): 753–9. doi:10.1016/S0968-0896(02)00473-X. PMID 12538005.
- ↑ Mattson RJ, Catt JD, Keavy D; et al. (2003). "Indanyl piperazines as melatonergic MT2 selective agents". Bioorg. Med. Chem. Lett. 13 (6): 1199–202. doi:10.1016/S0960-894X(03)00090-8. PMID 12643943.
