Target Information
Target General Infomation | |||||
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Target ID |
T20331
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Former ID |
TTDC00089
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Target Name |
Neuropeptide Y receptor 5
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Gene Name |
NPY5R
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Synonyms |
NPY-Y5 receptor; NPY5-R; NPYY5; Neuropeptide Y (NPY) Y(5) receptor; Neuropeptide Y receptor Y5; Y5 receptor; NPY5R
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Target Type |
Discontinued
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T20331
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UniProt ID | |||||
Sequence |
MDLELDEYYNKTLATENNTAATRNSDFPVWDDYKSSVDDLQYFLIGLYTFVSLLGFMGNL
LILMALMKKRNQKTTVNFLIGNLAFSDILVVLFCSPFTLTSVLLDQWMFGKVMCHIMPFL QCVSVLVSTLILISIAIVRYHMIKHPISNNLTANHGYFLIATVWTLGFAICSPLPVFHSL VELQETFGSALLSSRYLCVESWPSDSYRIAFTISLLLVQYILPLVCLTVSHTSVCRSISC GLSNKENRLEENEMINLTLHPSKKSGPQVKLSGSHKWSYSFIKKHRRRYSKKTACVLPAP ERPSQENHSRILPENFGSVRSQLSSSSKFIPGVPTCFEIKPEENSDVHELRVKRSVTRIK KRSRSVFYRLTILILVFAVSWMPLHLFHVVTDFNDNLISNRHFKLVYCICHLLGMMSCCL NPILYGFLNNGIKADLVSLIHCLHM |
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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 | |||||
References | |||||
Ref 532488 | New and emerging drug molecules against obesity. J Cardiovasc Pharmacol Ther. 2014 Jan;19(1):65-76. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536225 | Emerging 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 525809 | L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem Biophys Res Commun. 2000 May 27;272(1):169-73. | ||||
Ref 526277 | Bioorg 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 526683 | Development 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 527629 | Bioorg 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 527988 | Pharmacological 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 529977 | Bioorg 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 535122 | Neuropeptide 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 535534 | Bis(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 536091 | Neuropeptide Y induced modulation of dopamine synthesis in the striatum. Regul Pept. 2005 Jul 15;129(1-3):73-8. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536225 | Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. | ||||
Ref 536383 | Neuropeptide 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. |
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