Melatonin receptor 1B

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Melatonin receptor 1B
Identifiers
Symbols MTNR1B; MT2; MEL-1B-R
External IDs OMIM: 600804 MGI: 2181726 HomoloGene: 4350
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 4544 244701
Ensembl ENSG00000134640 ENSMUSG00000050901
Uniprot P49286 P70329
Refseq NM_005959 (mRNA)
NP_005950 (protein)		 NM_145712 (mRNA)
NP_663758 (protein)
Location 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 human gene.[1]

This gene encodes 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 although 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]

Contents

MT2R Ligands

The following MT2R ligands have selectivity over MT1R:

  • Compound 3d: antagonist with sub-nM affinity[2]
  • Compound 18f: antagonist and compound 18g partial agonist: sub-nM affinity, >100-fold selectivity over MT1[3]
  • Compound 14: antagonist[4]
  • Compound 13: agonist[5]

See also


References

  1. ^ a b "Entrez Gene: MTNR1B melatonin receptor 1B".
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. PMID 12538005. 
  5. ^ Mattson RJ, Catt JD, Keavy D, et al (2003). "Indanyl piperazines as melatonergic MT2 selective agents". Bioorg. Med. Chem. Lett. 13 (6): 1199–202. PMID 12643943. 

Further reading

  • Brzezinski A (1997). "Melatonin in humans.". N. Engl. J. Med. 336 (3): 186–95. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 
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v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
α1 (A, B, D), α2 (A, B, C), β1, β2, β3
CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin (DP, EP (1, 2, 3, 4), PGF), Prostacyclin, Thromboxane
B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182)
Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - neuromedin (B, U (1, 2)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like
Class C: Metabotropic
glutamate / pheromone
Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened

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