Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT24DGP)

• DTT Name: P2Y purinoceptor 4 (P2RY4)
• Synonyms: Uridine nucleotide receptor; UNR; P2Y4; P2P; NRU
• Gene Name: P2RY4
• DTT Type: Discontinued target; [1]
• UniProt ID: P2RY4_HUMAN
• TTD ID: T82083
• Sequence:
  MASTESSLLRSLGLSPGPGSSEVELDCWFDEDFKFILLPVSYAVVFVLGLGLNAPTLWLF
  IFRLRPWDATATYMFHLALSDTLYVLSLPTLIYYYAAHNHWPFGTEICKFVRFLFYWNLY
  CSVLFLTCISVHRYLGICHPLRALRWGRPRLAGLLCLAVWLVVAGCLVPNLFFVTTSNKG
  TTVLCHDTTRPEEFDHYVHFSSAVMGLLFGVPCLVTLVCYGLMARRLYQPLPGSAQSSSR
  LRSLRTIAVVLTVFAVCFVPFHITRTIYYLARLLEADCRVLNIVNVVYKVTRPLASANSC
  LDPVLYLLTGDKYRRQLRQLCGGGKPQPRTAASSLALVSLPEDSSCRWAATPQDSSCSTP
  RADRL
• Function: Receptor for UTP and UDP coupled to G-proteins that activate a phosphatidylinositol-calcium second messenger system. Not activated by ATP or ADP.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Taste transduction (hsa04742)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  P2Y receptors (R-HSA-417957)

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INS 316	DMTHMEI	Lung cancer	2C25.0	Discontinued in Phase 3	[1]

9 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(N)methanocarba-UTP	DM6SV7I	Discovery agent	N.A.	Investigative	[2]
2-amino-uridine-5'-monophosphate	DMO792L	Discovery agent	N.A.	Investigative	[3]
CTP	DM4T62U	Discovery agent	N.A.	Investigative	[1]
ITP	DMVFITX	Discovery agent	N.A.	Investigative	[1]
MRS2927	DMB2A7Q	Discovery agent	N.A.	Investigative	[4]
MRS4062	DMWKXGP	Discovery agent	N.A.	Investigative	[4]
N4-phenylethoxycytidine-5'-triphosphate	DM7KX2V	Discovery agent	N.A.	Investigative	[4]
PPADS	DMWHN3T	Discovery agent	N.A.	Investigative	[5]
UTPgammaS	DMKLB4O	Discovery agent	N.A.	Investigative	[6]

References

• [1] ATP, an agonist at the rat P2Y(4) receptor, is an antagonist at the human P2Y(4) receptor. Mol Pharmacol. 2000 May;57(5):926-31.
• [2] Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors. J Med Chem. 2002 Jan 3;45(1):208-18.
• [3] Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2011 Apr 28;54(8):2878-90.
• [4] Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate delta-ester modifications as selective agonists of the P2Y(4) receptor. J Med Chem. 2011 Jun 23;54(12):4018-33.
• [5] Development of selective agonists and antagonists of P2Y receptors. Purinergic Signal. 2009 Mar;5(1):75-89.
• [6] Enzymatic synthesis of UTP gamma S, a potent hydrolysis resistant agonist of P2U-purinoceptors. Br J Pharmacol. 1996 Jan;117(1):203-9.