Target Information
Target General Infomation | |||||
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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 | [536122] |
NEUROPEPTIDE-Y | Drug Info | Discontinued in Phase 2 | Discovery agent | [522433] | |
PYY3-36 | Drug Info | Discontinued in Phase 2 | Obesity | [536372], [538947] | |
TM30338 | Drug Info | Discontinued in Phase 2 | Obesity | [548209] | |
AC-162352 | Drug Info | Discontinued in Phase 1 | Obesity | [536122] | |
Agonist | AC-162352 | Drug Info | [536122] | ||
PD-4048 | Drug Info | [543757] | |||
PYY3-36 | Drug Info | [536122] | |||
Inhibitor | AcNPY(25-36) | Drug Info | [528484] | ||
AcPYY(22-36) | Drug Info | [528484] | |||
AcPYY(25-36) | Drug Info | [528484] | |||
AcPYY(26-36) | Drug Info | [528484] | |||
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 | Drug Info | [528136] | |||
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 | Drug Info | [528136] | |||
LRHYLNLLTRQRY-NH2 | Drug Info | [528667] | |||
NEUROPEPTIDE-Y | Drug Info | [529789] | |||
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
PYY(22-36) | Drug Info | [528484] | |||
PYY(25-36) | Drug Info | [528484] | |||
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 | Drug Info | [528136] | |||
Antagonist | BIIE0246 | Drug Info | [526081] | ||
BMS-192548 | Drug Info | [536122] | |||
JNJ-5207787 | Drug Info | [526883] | |||
Modulator | PEGylated PYY-3-36 | Drug Info | [543757] | ||
TM30338 | Drug Info | ||||
Pathways | |||||
References | |||||
Ref 522433 | ClinicalTrials.gov (NCT00748956) Intranasal Administration of Neuropeptide Y in Healthy Male Volunteers. U.S. National Institutes of Health. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536372 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | ||||
Ref 526081 | 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 526883 | 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. | ||||
Ref 528136 | 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 528484 | Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists. | ||||
Ref 528667 | 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 529789 | 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. |
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