Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T10670
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| Former ID |
TTDC00040
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| Target Name |
Neuropeptide Y receptor type 2
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| Gene Name |
NPY2R
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| Synonyms |
NPY-Y2 receptor; NPY2-R; Y2 receptor; NPY2R
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| Target Type |
Clinical Trial
|
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| Disease | Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | ||||
| Metabolic disorders [ICD9: 270-279; ICD10: E70-E89] | |||||
| Obesity [ICD9: 278; ICD10: E66] | |||||
| Function |
Receptor for neuropeptide Y andpeptide YY. The rank order of affinity of this receptor for pancreatic polypeptides is PYY > NPY > PYY (3-36) > NPY (2-36) > [Ile-31, Gln-34] PP > [Leu- 31, Pro-34] NPY > PP, [Pro-34] PYY and NPY free acid.
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| BioChemical Class |
GPCR rhodopsin
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| Target Validation |
T10670
|
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| UniProt ID | |||||
| Sequence |
MGPIGAEADENQTVEEMKVEQYGPQTTPRGELVPDPEPELIDSTKLIEVQVVLILAYCSI
ILLGVIGNSLVIHVVIKFKSMRTVTNFFIANLAVADLLVNTLCLPFTLTYTLMGEWKMGP VLCHLVPYAQGLAVQVSTITLTVIALDRHRCIVYHLESKISKRISFLIIGLAWGISALLA SPLAIFREYSLIEIIPDFEIVACTEKWPGEEKSIYGTVYSLSSLLILYVLPLGIISFSYT RIWSKLKNHVSPGAANDHYHQRRQKTTKMLVCVVVVFAVSWLPLHAFQLAVDIDSQVLDL KEYKLIFTVFHIIAMCSTFANPLLYGWMNSNYRKAFLSAFRCEQRLDAIHSEVSVTFKAK KNLEVRKNSGPNDSFTEATNV |
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| Drugs and Mode of Action | |||||
| Drug(s) | BMS-192548 | Drug Info | Preclinical | Obesity | [1] |
| NEUROPEPTIDE-Y | Drug Info | Discontinued in Phase 2 | Discovery agent | [2] | |
| PYY3-36 | Drug Info | Discontinued in Phase 2 | Obesity | [3], [4] | |
| TM30338 | Drug Info | Discontinued in Phase 2 | Obesity | [5] | |
| AC-162352 | Drug Info | Discontinued in Phase 1 | Obesity | [1] | |
| Agonist | AC-162352 | Drug Info | [1] | ||
| PD-4048 | Drug Info | [6] | |||
| PYY3-36 | Drug Info | [1] | |||
| Inhibitor | AcNPY(25-36) | Drug Info | [7] | ||
| AcPYY(22-36) | Drug Info | [7] | |||
| AcPYY(25-36) | Drug Info | [7] | |||
| AcPYY(26-36) | Drug Info | [7] | |||
| Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [8] | |||
| H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 | Drug Info | [8] | |||
| H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 | Drug Info | [8] | |||
| LRHYLNLLTRQRY-NH2 | Drug Info | [9] | |||
| NEUROPEPTIDE-Y | Drug Info | [10] | |||
| Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [8] | |||
| PYY(22-36) | Drug Info | [7] | |||
| PYY(25-36) | Drug Info | [7] | |||
| Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [8] | |||
| Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 | Drug Info | [8] | |||
| Antagonist | BIIE0246 | Drug Info | [11] | ||
| BMS-192548 | Drug Info | [1] | |||
| JNJ-5207787 | Drug Info | [12] | |||
| Modulator | PEGylated PYY-3-36 | Drug Info | [6] | ||
| TM30338 | Drug Info | ||||
| Pathways | |||||
| KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
| Reactome | Peptide ligand-binding receptors | ||||
| G alpha (i) signalling events | |||||
| WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
| Peptide GPCRs | |||||
| GPCR ligand binding | |||||
| GPCR downstream signaling | |||||
| References | |||||
| REF 1 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
| REF 2 | ClinicalTrials.gov (NCT00748956) Intranasal Administration of Neuropeptide Y in Healthy Male Volunteers. U.S. National Institutes of Health. | ||||
| REF 3 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | ||||
| REF 4 | (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: 1554). | ||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023122) | ||||
| REF 6 | (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. (Target id: 306). | ||||
| REF 7 | Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists. | ||||
| REF 8 | J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity. | ||||
| REF 9 | Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9. Epub 2007 Jan 24.A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice. | ||||
| REF 10 | J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. | ||||
| REF 11 | The peptide YY-preferring receptor mediating inhibition of small intestinal secretion is a peripheral Y(2) receptor: pharmacological evidence and molecular cloning. Mol Pharmacol. 2001 Jul;60(1):124-34. | ||||
| REF 12 | Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor. J Pharmacol Exp Ther. 2004 Mar;308(3):1130-7. Epub 2003 Nov 14. | ||||
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