Target Information

Target General Infomation
Target ID
T20331
Former ID
TTDC00089
Target Name
Neuropeptide Y receptor 5
Gene Name
NPY5R
Synonyms
NPY-Y5 receptor; NPY5-R; NPYY5; Neuropeptide Y (NPY) Y(5) receptor; Neuropeptide Y receptor Y5; Y5 receptor; NPY5R
Target Type
Discontinued
Disease Eating disorder; Obesity [ICD9: 278, 307.5; ICD10: E66, F50]
Eating disorders reduction in food intake [ICD9: 307.5; ICD10: F50]
Eating disorder; Obesity; Diabetes [ICD9: 250, 278, 307.5; ICD10: E08-E13, E66, F50]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Obesity [ICD9: 278; ICD10: E66]
Function
Receptor for neuropeptide Y and peptide YY. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity. Seems to be associated with food intake. Could be involved in feeding disorders.
BioChemical Class
GPCR rhodopsin
Target Validation
T20331
UniProt ID
Q15761
Sequence
MDLELDEYYNKTLATENNTAATRNSDFPVWDDYKSSVDDLQYFLIGLYTFVSLLGFMGNL
LILMALMKKRNQKTTVNFLIGNLAFSDILVVLFCSPFTLTSVLLDQWMFGKVMCHIMPFL
QCVSVLVSTLILISIAIVRYHMIKHPISNNLTANHGYFLIATVWTLGFAICSPLPVFHSL
VELQETFGSALLSSRYLCVESWPSDSYRIAFTISLLLVQYILPLVCLTVSHTSVCRSISC
GLSNKENRLEENEMINLTLHPSKKSGPQVKLSGSHKWSYSFIKKHRRRYSKKTACVLPAP
ERPSQENHSRILPENFGSVRSQLSSSSKFIPGVPTCFEIKPEENSDVHELRVKRSVTRIK
KRSRSVFYRLTILILVFAVSWMPLHLFHVVTDFNDNLISNRHFKLVYCICHLLGMMSCCL
NPILYGFLNNGIKADLVSLIHCLHM
Drugs and Mode of Action
Drug(s) FR-79620 Drug Info Preclinical Eating disorder; Obesity; Diabetes [536122]
GW-594884A Drug Info Preclinical Obesity [536122]
NPY antagonist Drug Info Preclinical Obesity [536122]
NPY5RA-972 Drug Info Preclinical Obesity [536122]
CGP71683A Drug Info Discontinued in Phase 3 Obesity [538948], [546849]
Velneperit Drug Info Discontinued in Phase 2 Obesity [532488]
Axovan-3 Drug Info Discontinued in Phase 1 Eating disorder; Obesity [536225]
S-234462 Drug Info Discontinued in Phase 1 Obesity [551685]
Inhibitor 2,4,4-triphenylimidazoline Drug Info [529977]
AR-129330 Drug Info [527629]
FR-226928 Drug Info [526277]
FR-230481 Drug Info [526277]
FR-233118 Drug Info [526277]
FR-73966 Drug Info [526277]
Antagonist Axovan-3 Drug Info [536225]
CGP71683A Drug Info [535122], [536091], [536383]
FMS586 Drug Info [527988]
FR-79620 Drug Info [536122]
GW-594884A Drug Info [536122]
JCF 109 Drug Info [526683]
L-152,804 Drug Info [525809]
LU-AA33810 Drug Info [543759]
NPY antagonist Drug Info [536122]
NPY Y5 antagonists Drug Info [543759]
NPY5RA-972 Drug Info [536122]
RJW-57926 Drug Info [536225]
S-19528 Drug Info [536225]
S-234462 Drug Info [551685]
S-25585 Drug Info [536225]
Velneperit Drug Info [551685]
Agonist Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)] Drug Info [535534]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP 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 532488New and emerging drug molecules against obesity. J Cardiovasc Pharmacol Ther. 2014 Jan;19(1):65-76.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536225Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36.
Ref 538948(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: 1562).
Ref 546849Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010609)
Ref 551685Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 525809L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem Biophys Res Commun. 2000 May 27;272(1):169-73.
Ref 526277Bioorg Med Chem Lett. 2002 Mar 11;12(5):799-802.Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 3: 7-methoxy-1-hydroxy-1-substituted tetraline derivatives.
Ref 526683Development and characterization of a highly selective neuropeptide Y Y5 receptor agonist radioligand: [125I][hPP1-17, Ala31, Aib32]NPY. Br J Pharmacol. 2003 Aug;139(7):1360-8.
Ref 527629Bioorg Med Chem Lett. 2005 Sep 1;15(17):3853-6.Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Ref 527988Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor. J Pharmacol Exp Ther. 2006 May;317(2):562-70. Epub 2006 Jan 25.
Ref 529977Bioorg Med Chem Lett. 2009 Mar 15;19(6):1670-4. Epub 2009 Feb 4.Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists.
Ref 535122Neuropeptide Y Y(5) receptor antagonist CGP71683A: the effects on food intake and anxiety-related behavior in the rat. Eur J Pharmacol. 2001 Mar 2;414(2-3):215-24.
Ref 535534Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)]: a neuropeptide Y (NPY) Y(5) receptor selective agonist with a latent stimulatory effect on food intake in rats. Peptides. 2002 Aug;23(8):1485-90.
Ref 536091Neuropeptide Y induced modulation of dopamine synthesis in the striatum. Regul Pept. 2005 Jul 15;129(1-3):73-8.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536225Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36.
Ref 536383Neuropeptide Y-induced enhancement of the evoked release of newly synthesized dopamine in rat striatum: mediation by Y2 receptors. Neuropharmacology. 2007 May;52(6):1396-402. Epub 2007 Feb 20.
Ref 543759(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: 308).
Ref 551685Clinical pipeline report, company report or official report of Shionogi (2011).

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.