Biology:Melatonin receptor 1A

Short description: Protein-coding gene in the species Homo sapiens

Generic protein structure example

Melatonin receptor type 1A is a protein that in humans is encoded by the MTNR1A gene.

Function

This gene encodes the MT₁ protein, one of two high-affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. This receptor is a G protein-coupled, 7-transmembrane receptor that is responsible for melatonin effects on mammalian circadian rhythm and reproductive alterations affected by day length. The receptor is an integral membrane protein that is readily detectable and localized to two specific regions of the brain. The hypothalamic suprachiasmatic nucleus appears to be involved in circadian rhythm while the hypophysial pars tuberalis may be responsible for the reproductive effects of melatonin.

Ligands

1. Melatonin – full agonist
2. Afobazole – agonist
3. Agomelatine – agonist

See also

• Melatonin receptor
• Discovery and development of melatonin receptor agonists

Further reading

• "Melatonin in humans". The New England Journal of Medicine 336 (3): 186–95. Jan 1997. doi:10.1056/NEJM199701163360306. PMID 8988899. 
• "Physical therapy and exercise-induced bronchospasm". Physical Therapy 55 (8): 878–81. Aug 1975. doi:10.1093/ptj/55.8.878. PMID 1144527. 
• "Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses". Neuron 13 (5): 1177–85. Nov 1994. doi:10.1016/0896-6273(94)90055-8. PMID 7946354. 
• "Characterization and regulation of the human ML1A melatonin receptor stably expressed in Chinese hamster ovary cells". Molecular Pharmacology 50 (1): 166–74. Jul 1996. PMID 8700109. 
• "Physiological exposure to melatonin supersensitizes the cyclic adenosine 3',5'-monophosphate-dependent signal transduction cascade in Chinese hamster ovary cells expressing the human mt1 melatonin receptor". Endocrinology 139 (7): 3064–71. Jul 1998. doi:10.1210/endo.139.7.6102. PMID 9645677. 
• "Alleic variants of human melatonin 1a receptor: function and prevalence in subjects with circadian rhythm sleep disorders". Biochemical and Biophysical Research Communications 262 (3): 832–7. Sep 1999. doi:10.1006/bbrc.1999.1308. PMID 10471411. 
• "Dual signaling of human Mel1a melatonin receptors via G(i2), G(i3), and G(q/11) proteins". Molecular Endocrinology 13 (12): 2025–38. Dec 1999. doi:10.1210/me.13.12.2025. PMID 10598579. 
• "Melatonin receptor mRNA expression in human granulosa cells". Molecular and Cellular Endocrinology 156 (1–2): 107–10. Oct 1999. doi:10.1016/S0303-7207(99)00135-5. PMID 10612428. 
• "CNS sympathetic outflow neurons to white fat that express MEL receptors may mediate seasonal adiposity". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology 281 (2): R666–72. Aug 2001. doi:10.1152/ajpregu.2001.281.2.R666. PMID 11448873. 
• "Cyclical regulation of GnRH gene expression in GT1-7 GnRH-secreting neurons by melatonin". Endocrinology 142 (11): 4711–20. Nov 2001. doi:10.1210/en.142.11.4711. PMID 11606436. 
• "Increased melatonin 1a-receptor immunoreactivity in the hippocampus of Alzheimer's disease patients". Journal of Pineal Research 32 (1): 59–62. Jan 2002. doi:10.1034/j.1600-079x.2002.00841.x. PMID 11841602. 
• "Distribution of melatonin MT1 receptor immunoreactivity in human retina". The Journal of Histochemistry and Cytochemistry 50 (4): 519–26. Apr 2002. doi:10.1177/002215540205000408. PMID 11897804. 
• "Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer". The Journal of Biological Chemistry 277 (24): 21522–8. Jun 2002. doi:10.1074/jbc.M200729200. PMID 11940583. 
• "MT(1) melatonin receptor overexpression enhances the growth suppressive effect of melatonin in human breast cancer cells". Molecular and Cellular Endocrinology 192 (1–2): 147–56. Jun 2002. doi:10.1016/S0303-7207(02)00029-1. PMID 12088876. 
• "Functional activity of serotoninergic and melatoninergic systems expressed in the skin". Journal of Cellular Physiology 196 (1): 144–53. Jul 2003. doi:10.1002/jcp.10287. PMID 12767050. 
• "Allelic variants of human melatonin 1A receptor in patients with familial adolescent idiopathic scoliosis". Spine 28 (17): 2025–8; discussion 2029. Sep 2003. doi:10.1097/01.BRS.0000083235.74593.49. PMID 12973153. 
• "The melatonin receptor subtype MT1 is expressed in human gallbladder epithelia". Journal of Pineal Research 36 (1): 43–8. Jan 2004. doi:10.1046/j.1600-079X.2003.00095.x. PMID 14675129.