Target Information

Target General Infomation
Target ID
T10670
Former ID
TTDC00040
Target Name
Neuropeptide Y receptor type 2
Gene Name
NPY2R
Synonyms
NPY-Y2 receptor; NPY2-R; Y2 receptor; NPY2R
Target Type
Clinical Trial
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T10670
UniProt ID
P49146
Sequence
MGPIGAEADENQTVEEMKVEQYGPQTTPRGELVPDPEPELIDSTKLIEVQVVLILAYCSI
ILLGVIGNSLVIHVVIKFKSMRTVTNFFIANLAVADLLVNTLCLPFTLTYTLMGEWKMGP
VLCHLVPYAQGLAVQVSTITLTVIALDRHRCIVYHLESKISKRISFLIIGLAWGISALLA
SPLAIFREYSLIEIIPDFEIVACTEKWPGEEKSIYGTVYSLSSLLILYVLPLGIISFSYT
RIWSKLKNHVSPGAANDHYHQRRQKTTKMLVCVVVVFAVSWLPLHAFQLAVDIDSQVLDL
KEYKLIFTVFHIIAMCSTFANPLLYGWMNSNYRKAFLSAFRCEQRLDAIHSEVSVTFKAK
KNLEVRKNSGPNDSFTEATNV
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
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 522433ClinicalTrials.gov (NCT00748956) Intranasal Administration of Neuropeptide Y in Healthy Male Volunteers. U.S. National Institutes of Health.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536372Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.
Ref 538947(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 548209Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023122)
Ref 526081The 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 526883Characterization 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 528136J 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 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528667Bioorg 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 529789J 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 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 543757(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).

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