Synonyms
Melatonin receptor MT1:
Mel1a; Mel1A; Melatonin 1 receptor; Melatonin receptor 1A; Melatonin receptor MT1; ML1A; MT(1) receptor; MT1 melatonin receptor; MT1 receptor; MT1R; Mtnr1a
Melatonin receptor MT2:
Mel1b; Mel1B; Melatonin 2 receptor; Melatonin receptor 1B; Melatonin receptor MT2; ML1B; MT(2) receptor; MT2 receptor; MT2R; Mtnr1b
Historical Background
Melatonin (N-acetyl-5-methoxytryptamine) is an evolutionary old molecule which is derived from the essential amino acid tryptophan in a four-step biosynthesis pathway. Melatonin is synthesized by many organisms as diverse as bacteria, protists, fungi, macroalgae, plants, and animals. During evolution, several functions of melatonin appeared including protection of cells against oxidative stress, regulation of circadian rhythmicity, and ciliary swimming in invertebrates. The function of melatonin further expanded in mammals (see below). In mammals, the synthesis of melatonin is regulated by light and by the circadian activity...
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References
Ayoub MA, Couturier C, Lucas-Meunier E, Angers S, Fossier P, Bouvier M, et al. Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer. J Biol Chem. 2002;277:21522–8. doi:10.1074/jbc.M200729200.
Baba K, Benleulmi-Chaachoua A, Journe AS, Kamal M, Guillaume JL, Dussaud S, et al. Heteromeric MT1/MT2 melatonin receptors modulate photoreceptor function. Sci Signal. 2013;6:ra89. doi:10.1126/scisignal.2004302.
Bonnefond A, Clement N, Fawcett K, Yengo L, Vaillant E, Guillaume JL, et al. Rare MTNR1B variants impairing melatonin receptor 1B function contribute to type 2 diabetes. Nat Genet. 2012;44:297–301. doi:10.1038/ng.1053.
Dubocovich ML, Delagrange P, Krause DN, Sugden D, Cardinali DP, Olcese J. International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors. Pharmacol Rev. 2010;62:343–80.
Ebisawa T, Karne S, Lerner MR, Reppert SM. Expression cloning of a high-affinity melatonin receptor from Xenopus dermal melanophores. Proc Natl Acad Sci U S A. 1994;91:6133–7.
Jin X, von Gall C, Pieschl RL, Gribkoff VK, Stehle JH, Reppert SM, et al. Targeted disruption of the mouse Mel(1b) melatonin receptor. Mol Cell Biol. 2003;23:1054–60.
Jockers R, Delagrange P, Dubocovich ML, Markus RP, Renault N, Tosini G, et al. Update on melatonin receptors. IUPHAR Review. Br J Pharmacol. 2016. doi:10.1111/bph.13536.
Kamal M, Gbahou F, Guillaume JL, Daulat AM, Benleulmi-Chaachoua A, Luka M, et al. Convergence of melatonin and serotonin (5-HT) signaling at MT2/5-HT2C receptor heteromers. J Biol Chem. 2015;290:11537–46. doi:10.1074/jbc.M114.559542.
Lerner AB, Case JD, Biemann K, Heinzelman R, Szmuszkovicz J, Anthony W, et al. Isolation of 5-methoxyindole-3-acetic acid from bovine pineal glands. J Am Chem Soc. 1959a;81:5264. doi:10.1021/ja01528a064.
Lerner AB, Case JD, Heinzelman RV. Structure of melatonin. J Am Chem Soc. 1959b;81:6084–5. doi:10.1021/ja01531a060.
Levoye A, Dam J, Ayoub MA, Guillaume JL, Couturier C, Delagrange P, et al. The orphan GPR50 receptor specifically inhibits MT1 melatonin receptor function through heterodimerization. EMBO J. 2006;25:3012–23. doi:10.1038/sj.emboj.7601193.
Liu C, Weaver DR, Jin X, Shearman LP, Pieschl RL, Gribkoff VK, et al. Molecular dissection of two distinct actions of melatonin on the suprachiasmatic circadian clock. Neuron. 1997;19:91–102.
Liu J, Clough SJ, Hutchinson AJ, Adamah-Biassi EB, Popovska-Gorevski M, Dubocovich ML. MT1 and MT2 melatonin receptors: a therapeutic perspective. Annu Rev Pharmacol Toxicol. 2016;56:361–83. doi:10.1146/annurev-pharmtox-010814-124742.
Reppert SM, Weaver DR, Ebisawa T. Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses. Neuron. 1994;13:1177–85. doi: http://dx.doi.org/10.1016/0896-6273(94)90055-8.
Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF. Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel(1b) melatonin receptor. Proc Natl Acad Sci U S A. 1995;92:8734–8.
Tosini G, Owino S, Guillaume JL, Jockers R. Understanding melatonin receptor pharmacology: latest insights from mouse models, and their relevance to human disease. BioEssays : News Rev Mol Cell Dev Biol. 2014;36:778–87. doi:10.1002/bies.201400017.
Zlotos DP, Jockers R, Cecon E, Rivara S, Witt-Enderby PA. MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014;57:3161–85. doi:10.1021/jm401343c.
Acknowledgments
We would like to acknowledge Dr. Erika Cecon for reading the manuscript and helpful suggestions.
This work was supported by the Fondation de la Recherche Médicale (Equipe FRM DEQ20130326503), Institut National de la Santé et de la Recherche Médicale (INSERM), Centre National de la Recherche Scientifique (CNRS) and the “Who am I?” laboratory of excellence No.ANR-11-LABX-0071 funded by the French Government through its “Investments for the Future” program operated by the French National Research Agency (ANR) under grant No.ANR-11-IDEX-0005-01.
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Oishi, A., Jockers, R. (2018). Melatonin Receptor MT1 and MT2. In: Choi, S. (eds) Encyclopedia of Signaling Molecules. Springer, Cham. https://doi.org/10.1007/978-3-319-67199-4_101751
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