Target Information

Target General Infomation
Target ID
T48268
Former ID
TTDS00422
Target Name
Melatonin receptor type 1B
Gene Name
MTNR1B
Synonyms
Mel-1B-R; Mel1b melatonin receptor; MTNR1B
Target Type
Successful
Disease Circadian rhythm sleep disorder [ICD9: 327.3, 780.55; ICD10: G47.2]
Epilepsy [ICD10: G40]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Function
High affinityreceptor for melatonin. Likely to mediates the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity.
BioChemical Class
GPCR rhodopsin
Target Validation
T48268
UniProt ID
P49286
Sequence
MSENGSFANCCEAGGWAVRPGWSGAGSARPSRTPRPPWVAPALSAVLIVTTAVDVVGNLL
VILSVLRNRKLRNAGNLFLVSLALADLVVAFYPYPLILVAIFYDGWALGEEHCKASAFVM
GLSVIGSVFNITAIAINRYCYICHSMAYHRIYRRWHTPLHICLIWLLTVVALLPNFFVGS
LEYDPRIYSCTFIQTASTQYTAAVVVIHFLLPIAVVSFCYLRIWVLVLQARRKAKPESRL
CLKPSDLRSFLTMFVVFVIFAICWAPLNCIGLAVAINPQEMAPQIPEGLFVTSYLLAYFN
SCLNAIVYGLLNQNFRREYKRILLALWNPRHCIQDASKGSHAEGLQSPAPPIIGVQHQAD
AL
Drugs and Mode of Action
Drug(s) Ramelteon Drug Info Approved Insomnia [536647], [538833]
Tasimelteon Drug Info Approved Insomnia [542414], [551871]
VLB-01 Drug Info Phase 3 Epilepsy [549135]
Ramelteon Drug Info Terminated Circadian rhythm sleep disorder [536647], [538833]
Inhibitor 5-methoxycarbonylamino-N-acetyltryptamine Drug Info [529396]
Beta,beta-dimethylmelatonin Drug Info [528234]
Beta-methylmelatonin Drug Info [528234]
IODOMELATONIN Drug Info [526317]
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide Drug Info [551266]
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide Drug Info [529396]
N-(3-(2,5-dimethoxyphenyl)propyl)acetamide Drug Info [530786]
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide Drug Info [530786]
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide Drug Info [530786]
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide Drug Info [529949]
N-(3-(3-methoxyphenyl)propyl)acetamide Drug Info [530786]
N-(3-(3-methoxyphenyl)propyl)propionamide Drug Info [530786]
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide Drug Info [530786]
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide Drug Info [530786]
N-(3-Benzooxazol-7-yl-propyl)-acetamide Drug Info [527111]
N-(3-Benzooxazol-7-yl-propyl)-butyramide Drug Info [527111]
N-(3-Benzooxazol-7-yl-propyl)-propionamide Drug Info [527111]
N-[3-(2-Ethyl-benzooxazol-7-yl)-propyl]-acetamide Drug Info [527111]
UCM-454 Drug Info [529949]
Modulator Ramelteon Drug Info [529337], [532551]
VLB-01 Drug Info [1572591]
Agonist Tasimelteon Drug Info [542414]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Circadian entrainment
Reactome Class A/1 (Rhodopsin-like receptors)
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Small Ligand GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 536647Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
Ref 538833(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1356).
Ref 542414(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7393).
Ref 549135Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032715)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 526317J Med Chem. 2002 Apr 25;45(9):1853-9.Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).
Ref 527111Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Ref 528234J Med Chem. 2006 Jun 15;49(12):3509-19.Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines.
Ref 529337Ramelteon: a melatonin receptor agonist for the treatment of insomnia. J Postgrad Med. 2008 Jan-Mar;54(1):45-8.
Ref 529396Bioorg Med Chem. 2008 May 1;16(9):4954-62. Epub 2008 Mar 17.Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.
Ref 529949J Med Chem. 2009 Feb 12;52(3):826-33.2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists.
Ref 530786Bioorg Med Chem Lett. 2010 Apr 15;20(8):2582-5. Epub 2010 Feb 25.Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands.
Ref 532551MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014 Apr 24;57(8):3161-85.
Ref 542414(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7393).
Ref 551266Mapping the melatonin receptor. 2. synthesis and biological activity of indole derived melatonin analogues with restricted conformations of the C-3 amidoethane side chain, Bioorg. Med. Chem. Lett. 4(13):1559-1564 (1994).
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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