Target Information

Target General Infomation
Target ID
T27944
Former ID
TTDC00043
Target Name
Neuropeptide Y receptor type 4
Gene Name
NPY4R
Synonyms
NPY4-R; PP1; PPYR1; Pancreatic polypeptide receptor 1; NPY4R
Target Type
Clinical Trial
Disease Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Obesity [ICD9: 278; ICD10: E66]
Schizophrenia [ICD9: 295; ICD10: F20]
Function
Receptor for neuropeptide Y and peptide YY. The rank order of affinity of this receptor for pancreatic polypeptides is PP, PP (2-36) and [Ile-31, Gln-34] PP > [Pro-34] PYY > PYY and [Leu-31, Pro-34] NPY > NPY > PYY (3-36) and NPY (2-36) > PP (13- 36) > PP (31-36) > NPY free acid.
BioChemical Class
GPCR rhodopsin
Target Validation
T27944
UniProt ID
P50391
Sequence
MNTSHLLALLLPKSPQGENRSKPLGTPYNFSEHCQDSVDVMVFIVTSYSIETVVGVLGNL
CLMCVTVRQKEKANVTNLLIANLAFSDFLMCLLCQPLTAVYTIMDYWIFGETLCKMSAFI
QCMSVTVSILSLVLVALERHQLIINPTGWKPSISQAYLGIVLIWVIACVLSLPFLANSIL
ENVFHKNHSKALEFLADKVVCTESWPLAHHRTIYTTFLLLFQYCLPLGFILVCYARIYRR
LQRQGRVFHKGTYSLRAGHMKQVNVVLVVMVVAFAVLWLPLHVFNSLEDWHHEAIPICHG
NLIFLVCHLLAMASTCVNPFIYGFLNTNFKKEIKALVLTCQQSAPLEESEHLPLSTVHTE
VSKGSLRLSGRSNPI
Drugs and Mode of Action
Drug(s) TM30338 Drug Info Discontinued in Phase 2 Obesity [548209]
TM30339 Drug Info Discontinued in Phase 2 Schizophrenia [522428]
Inhibitor 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]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info [528136]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info [528136]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 Drug Info [528136]
[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info [528136]
Agonist PD-4074 Drug Info [543758]
TM30339 Drug Info [536490]
[125I]GR231118 Drug Info [525704]
Modulator 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 522428ClinicalTrials.gov (NCT00746824) A Study to Determine the Effects of TM30339 on Weight Loss in Obese Individuals.. U.S. National Institutes of Health.
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 525704[(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors. Br J Pharmacol. 2000 Jan;129(1):37-46.
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 536490Neuropeptide y receptor selective ligands in the treatment of obesity. Endocr Rev. 2007 Oct;28(6):664-84.
Ref 543758(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: 307).

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