Melatonin receptor

melatonin receptor 1A
Identifiers
SymbolMTNR1A
NCBI gene4543
HGNC7463
OMIM600665
RefSeqNM_005958
UniProtP48039
Other data
LocusChr. 4 q35.1
Search for
StructuresSwiss-model
DomainsInterPro
melatonin receptor 1B
Identifiers
SymbolMTNR1B
NCBI gene4544
HGNC7464
OMIM600804
RefSeqNM_005959
UniProtP49286
Other data
LocusChr. 11 q21-q22
Search for
StructuresSwiss-model
DomainsInterPro

Melatonin receptors are G protein-coupled receptors (GPCR) which bind melatonin.[1] Three types of melatonin receptors have been cloned. The MT1 (or Mel1A or MTNR1A) and MT2 (or Mel1B or MTNR1B) receptor subtypes are present in humans and other mammals,[2] while an additional melatonin receptor subtype MT3 (or Mel1C or MTNR1C) has been identified in amphibia and birds.[3] The receptors are crucial in the signal cascade of melatonin. In the field of chronobiology, melatonin has been found to be a key player in the synchrony of biological clocks. Melatonin secretion by the pineal gland has circadian rhythmicity regulated by the suprachiasmatic nucleus (SCN) found in the brain. The SCN functions as the timing regulator for melatonin; melatonin then follows a feedback loop to decrease SCN neuronal firing. The receptors MT1 and MT2 control this process.[4] Melatonin receptors are found throughout the body in places such as the brain, the retina of the eye, the cardiovascular system, the liver and gallbladder, the colon, the skin, the kidneys, and many others.[5] In 2019, X-ray crystal and cryo-EM structures of MT1 and MT2 were reported.[6][7][8][9]

  1. ^ Reppert SM (December 1997). "Melatonin receptors: molecular biology of a new family of G protein-coupled receptors". Journal of Biological Rhythms. 12 (6): 528–531. doi:10.1177/074873049701200606. PMID 9406026. S2CID 6501856.
  2. ^ Reppert SM, Weaver DR, Godson C (March 1996). "Melatonin receptors step into the light: cloning and classification of subtypes". Trends in Pharmacological Sciences. 17 (3): 100–102. doi:10.1016/0165-6147(96)10005-5. PMID 8936344.
  3. ^ Sugden D, Davidson K, Hough KA, Teh MT (October 2004). "Melatonin, melatonin receptors and melanophores: a moving story". Pigment Cell Research. 17 (5): 454–460. doi:10.1111/j.1600-0749.2004.00185.x. PMID 15357831.
  4. ^ Doghramji K (August 2007). "Melatonin and its receptors: a new class of sleep-promoting agents". Journal of Clinical Sleep Medicine. 3 (5 Suppl): S17–S23. doi:10.5664/jcsm.26932. PMC 1978320. PMID 17824497.
  5. ^ Emet M, Ozcan H, Ozel L, Yayla M, Halici Z, Hacimuftuoglu A (June 2016). "A Review of Melatonin, Its Receptors and Drugs". The Eurasian Journal of Medicine. 48 (2): 135–141. doi:10.5152/eurasianjmed.2015.0267. PMC 4970552. PMID 27551178.
  6. ^ Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, et al. (May 2019). "Structural basis of ligand recognition at the human MT1 melatonin receptor". Nature. 569 (7755): 284–288. Bibcode:2019Natur.569..284S. doi:10.1038/s41586-019-1141-3. PMC 6696938. PMID 31019306.
  7. ^ Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, et al. (May 2019). "XFEL structures of the human MT2 melatonin receptor reveal the basis of subtype selectivity". Nature. 569 (7755): 289–292. Bibcode:2019Natur.569..289J. doi:10.1038/s41586-019-1144-0. PMC 6589158. PMID 31019305.
  8. ^ Stauch B, Johansson LC, Cherezov V (April 2020). "Structural insights into melatonin receptors". The FEBS Journal. 287 (8): 1496–1510. doi:10.1111/febs.15128. PMC 7174090. PMID 31693784.
  9. ^ Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, et al. (August 2021). "Cryo-EM structure of the human MT1-Gi signaling complex". Nature Structural & Molecular Biology. 28 (8): 694–701. doi:10.1038/s41594-021-00634-1. PMID 34354246. S2CID 236935241.