Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTW4N16)

• DTT Name: Neuropeptide Y receptor type 4 (NPY4R)
• Synonyms: Pancreatic polypeptide receptor 1; PPYR1; NPY4R; NPY4-R
• Gene Name: NPY4R
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: NPY4R_HUMAN
• TTD ID: T27944
• Sequence:
  MNTSHLLALLLPKSPQGENRSKPLGTPYNFSEHCQDSVDVMVFIVTSYSIETVVGVLGNL
  CLMCVTVRQKEKANVTNLLIANLAFSDFLMCLLCQPLTAVYTIMDYWIFGETLCKMSAFI
  QCMSVTVSILSLVLVALERHQLIINPTGWKPSISQAYLGIVLIWVIACVLSLPFLANSIL
  ENVFHKNHSKALEFLADKVVCTESWPLAHHRTIYTTFLLLFQYCLPLGFILVCYARIYRR
  LQRQGRVFHKGTYSLRAGHMKQVNVVLVVMVVAFAVLWLPLHVFNSLEDWHHEAIPICHG
  NLIFLVCHLLAMASTCVNPFIYGFLNTNFKKEIKALVLTCQQSAPLEESEHLPLSTVHTE
  VSKGSLRLSGRSNPI
• 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.
• KEGG Pathway: Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Peptide ligand-binding receptors (R-HSA-375276)

Molecular Interaction Atlas (MIA) of This DTT

2 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
TM30338	DMXNQLU	Obesity	5B81	Discontinued in Phase 2	[2]
TM30339	DMW7LQT	Schizophrenia	6A20	Discontinued in Phase 2	[1]

9 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2	DMVWM75	Discovery agent	N.A.	Investigative	[3]
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2	DM9XK05	Discovery agent	N.A.	Investigative	[3]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2	DMKH8PF	Discovery agent	N.A.	Investigative	[3]
PD-4074	DM4BDEY	Diabetic complication	5A2Y	Investigative	[4]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2	DMBERSG	Discovery agent	N.A.	Investigative	[3]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2	DM4SWQA	Discovery agent	N.A.	Investigative	[3]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2	DM56MOV	Discovery agent	N.A.	Investigative	[3]
[125I]GR231118	DMFWE4H	Discovery agent	N.A.	Investigative	[5]
[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2	DMWFGBC	Discovery agent	N.A.	Investigative	[3]

References

• [1] Neuropeptide y receptor selective ligands in the treatment of obesity. Endocr Rev. 2007 Oct;28(6):664-84.
• [2] Anti-Obesity Drug Discovery and Development, Atta-ur- Rahman, page(108)
• [3] Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar a... J Med Chem. 2006 Apr 20;49(8):2661-5.
• [4] URL: 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).
• [5] [(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.