Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T27944
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| Former ID |
TTDC00043
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| Target Name |
Neuropeptide Y receptor type 4
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| Gene Name |
NPY4R
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| Synonyms |
NPY4-R; PP1; PPYR1; Pancreatic polypeptide receptor 1; NPY4R
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| Target Type |
Clinical Trial
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| 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.
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| BioChemical Class |
GPCR rhodopsin
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| Target Validation |
T27944
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| UniProt ID | |||||
| Sequence |
MNTSHLLALLLPKSPQGENRSKPLGTPYNFSEHCQDSVDVMVFIVTSYSIETVVGVLGNL
CLMCVTVRQKEKANVTNLLIANLAFSDFLMCLLCQPLTAVYTIMDYWIFGETLCKMSAFI QCMSVTVSILSLVLVALERHQLIINPTGWKPSISQAYLGIVLIWVIACVLSLPFLANSIL ENVFHKNHSKALEFLADKVVCTESWPLAHHRTIYTTFLLLFQYCLPLGFILVCYARIYRR LQRQGRVFHKGTYSLRAGHMKQVNVVLVVMVVAFAVLWLPLHVFNSLEDWHHEAIPICHG NLIFLVCHLLAMASTCVNPFIYGFLNTNFKKEIKALVLTCQQSAPLEESEHLPLSTVHTE VSKGSLRLSGRSNPI |
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| Drugs and Mode of Action | |||||
| Drug(s) | TM30338 | Drug Info | Discontinued in Phase 2 | Obesity | [1] |
| TM30339 | Drug Info | Discontinued in Phase 2 | Schizophrenia | [2] | |
| Inhibitor | Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [3] | ||
| H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 | Drug Info | [3] | |||
| H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 | Drug Info | [3] | |||
| Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [3] | |||
| Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [3] | |||
| Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 | Drug Info | [3] | |||
| [Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2 | Drug Info | [3] | |||
| Agonist | PD-4074 | Drug Info | [4] | ||
| TM30339 | Drug Info | [5] | |||
| [125I]GR231118 | Drug Info | [6] | |||
| 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 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023122) | ||||
| REF 2 | ClinicalTrials.gov (NCT00746824) A Study to Determine the Effects of TM30339 on Weight Loss in Obese Individuals.. U.S. National Institutes of Health. | ||||
| REF 3 | 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 4 | (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). | ||||
| REF 5 | Neuropeptide y receptor selective ligands in the treatment of obesity. Endocr Rev. 2007 Oct;28(6):664-84. | ||||
| REF 6 | [(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. | ||||
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