Melatonin receptor 1B: Difference between revisions
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{{PBB|geneid=4544}} |
{{PBB|geneid=4544}} |
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'''Melatonin receptor 1B''', also known as '''MTNR1B''', is a |
'''Melatonin receptor 1B''', also known as '''MTNR1B''', is a [[protein]] which in humans is encoded by the ''MTNR1B'' [[gene]].<ref name="entrez">{{cite web | title = Entrez Gene: MTNR1B melatonin receptor 1B| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4544| accessdate = }}</ref><ref name="pmid7568007">{{cite journal | author = Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF | title = Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 92 | issue = 19 | pages = 8734–8 | year = 1995 | month = September | pmid = 7568007 | pmc = 41041 | doi = | url = http://www.pnas.org/cgi/pmidlookup?view=long&pmid=7568007 | issn = }}</ref> |
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== Function == |
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This gene encodes the MT<sub>2</sub> [[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 receptors|G-protein coupled]], 7-transmembrane receptor. It is found primarily in the [[retina]] and brain although this detection requires [[Reverse transcription polymerase chain reaction|RT-PCR]]. It is thought to participate in light-dependent functions in the retina and may be involved in the neurobiological effects of melatonin.<ref name="entrez">{{cite web | title = Entrez Gene: MTNR1B melatonin receptor 1B| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4544| accessdate = }}</ref> |
This gene encodes the MT<sub>2</sub> [[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 receptors|G-protein coupled]], 7-transmembrane receptor. It is found primarily in the [[retina]] and brain although this detection requires [[Reverse transcription polymerase chain reaction|RT-PCR]]. It is thought to participate in light-dependent functions in the retina and may be involved in the neurobiological effects of melatonin.<ref name="entrez">{{cite web | title = Entrez Gene: MTNR1B melatonin receptor 1B| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4544| accessdate = }}</ref> |
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== Clinical significance == |
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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.<ref name="SN1">{{cite web | title = Gene That Regulates Glucose Levels And Increases Risk For Diabetes Identified | url = http://www.sciencedaily.com/releases/2008/06/080609085957.htm}}</ref><ref name="SN2">{{cite web | title = Body Clock Linked To Diabetes And High Blood Sugar In New Genome-wide Study | url = http://www.sciencedaily.com/releases/2008/12/081207133817.htm}}</ref><ref name="SN3">{{cite web | title = Is There A Relationship Between Sleep-wake Rhythm And Diabetes? A New Gene Variant Influences Fasting Glucose Levels Via The Melatonin Metabolism | url = http://www.sciencedaily.com/releases/2009/01/090116073601.htm}}</ref> |
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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.<ref name="SN1">{{cite web | title = Gene That Regulates Glucose Levels And Increases Risk For Diabetes Identified | url = http://www.sciencedaily.com/releases/2008/06/080609085957.htm}}</ref><ref name="SN2">{{cite web | title = Body Clock Linked To Diabetes And High Blood Sugar In New Genome-wide Study | url = http://www.sciencedaily.com/releases/2008/12/081207133817.htm}}</ref><ref name="SN3">{{cite web | title = Is There A Relationship Between Sleep-wake Rhythm And Diabetes? A New Gene Variant Influences Fasting Glucose Levels Via The Melatonin Metabolism | url = http://www.sciencedaily.com/releases/2009/01/090116073601.htm}}</ref><ref name="pmid19060907">{{cite journal | author = Prokopenko I, Langenberg C, Florez JC, ''et al'' | title = Variants in MTNR1B influence fasting glucose levels | journal = Nat. Genet. | volume = 41 | issue = 1 | pages = 77–81 | year = 2009 | month = January | pmid = 19060907 | doi = 10.1038/ng.290 | url = | issn = }}</ref><ref name="pmid19060908">{{cite journal | author = Lyssenko V, Nagorny CL, Erdos MR, ''et al'' | title = Common variant in MTNR1B associated with increased risk of type 2 diabetes and impaired early insulin secretion | journal = Nat. Genet. | volume = 41 | issue = 1 | pages = 82–8 | year = 2009 | month = January | pmid = 19060908 | doi = 10.1038/ng.288 | url = | issn = }}</ref><ref name="pmid19060909">{{cite journal | author = Bouatia-Naji N, Bonnefond A, Cavalcanti-Proença C, ''et al'' | title = A variant near MTNR1B is associated with increased fasting plasma glucose levels and type 2 diabetes risk | journal = Nat. Genet. | volume = 41 | issue = 1 | pages = 89–94 | year = 2009 | month = January | pmid = 19060909 | doi = 10.1038/ng.277 | url = | issn = }}</ref><ref name="pmid19088850">{{cite journal | author = Staiger H, Machicao F, Schäfer SA, ''et al'' | title = Polymorphisms within the novel type 2 diabetes risk locus MTNR1B determine beta-cell function | journal = PLoS ONE | volume = 3 | issue = 12 | pages = e3962 | year = 2008 | pmid = 19088850 | pmc = 2597741 | doi = 10.1371/journal.pone.0003962 | url = | issn = }}</ref> |
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==MT2R Ligands== |
==MT2R Ligands== |
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==See also== |
==See also== |
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* [[Melatonin receptor]] |
* [[Melatonin receptor]] |
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{{-}} |
{{-}} |
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==References== |
==References== |
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Revision as of 22:45, 18 January 2009
Template:PBB Melatonin receptor 1B, also known as MTNR1B, is a protein which in humans is encoded by the MTNR1B gene.[1][2]
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 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]
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][6][7][8][9]
MT2R Ligands
The following MT2R ligands have selectivity over MT1R:
- Compound 3d: antagonist with sub-nM affinity[10]
- Compound 18f: antagonist and compound 18g partial agonist: sub-nM affinity, >100-fold selectivity over MT1[11]
- Compound 14: antagonist[12]
- Compound 13: agonist[13]
See also
References
- ^ a b "Entrez Gene: MTNR1B melatonin receptor 1B".
- ^ Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF (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. PMC 41041. PMID 7568007.
{{cite journal}}: Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ "Gene That Regulates Glucose Levels And Increases Risk For Diabetes Identified".
- ^ "Body Clock Linked To Diabetes And High Blood Sugar In New Genome-wide Study".
- ^ "Is There A Relationship Between Sleep-wake Rhythm And Diabetes? A New Gene Variant Influences Fasting Glucose Levels Via The Melatonin Metabolism".
- ^ Prokopenko I, Langenberg C, Florez JC; et al. (2009). "Variants in MTNR1B influence fasting glucose levels". Nat. Genet. 41 (1): 77–81. doi:10.1038/ng.290. PMID 19060907.
{{cite journal}}: Explicit use of et al. in:|author=(help); Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ Lyssenko V, Nagorny CL, Erdos MR; et al. (2009). "Common variant in MTNR1B associated with increased risk of type 2 diabetes and impaired early insulin secretion". Nat. Genet. 41 (1): 82–8. doi:10.1038/ng.288. PMID 19060908.
{{cite journal}}: Explicit use of et al. in:|author=(help); Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ Bouatia-Naji N, Bonnefond A, Cavalcanti-Proença C; et al. (2009). "A variant near MTNR1B is associated with increased fasting plasma glucose levels and type 2 diabetes risk". Nat. Genet. 41 (1): 89–94. doi:10.1038/ng.277. PMID 19060909.
{{cite journal}}: Explicit use of et al. in:|author=(help); Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ 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. PMID 19088850.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) CS1 maint: unflagged free DOI (link) - ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link)
External links
- "Melatonin Receptors: MT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
{{cite web}}: Cite has empty unknown parameter:|coauthors=(help)
Further reading
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.