Target intelligence / Profile preview

Pyrimidinergic receptor P2Y4 (P2Y4)

Target
P2Y4
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Pyrimidinergic receptor P2Y4 (P2Y4) is a G protein-coupled receptor (GPCR) that primarily responds to extracellular pyrimidine nucleotides, notably uridine triphosphate (UTP) and uridine diphosphate (UDP)[1][7]. It is only partially responsive to ATP and not activated by ADP[1][3][7]. P2Y4 is part of the P2Y receptor family, which mediates diverse cellular effects through the activation of G proteins, leading to phospholipase C stimulation, inositol phosphate generation, and increased intracellular calcium[2][7]. P2Y4 is implicated in purinergic signaling pathways relevant to epithelial transport, inflammation, neuronal signaling, and possibly cancer. The receptor forms functional oligomers on cell surfaces and its activation can trigger ERK phosphorylation and other secondary messenger cascades[2][7]. Endogenous ligands include UTP and UDP, with ATP acting as an antagonist in the human receptor. The receptor is a validated target for experimental tool compounds but is not a target of major marketed drugs as of current knowledge[7]. Diseases potentially associated with P2Y4 dysregulation include certain cancers and hereditary fibroproliferative disorders[1].

Other names
P2RY4P2Y purinoceptor 4NRUUNRP2Y4Rpyrimidinergic receptor P2Yuridine nucleotide receptorP2Y ATP receptor 4pyrimidinoceptor
02

Mechanism of action

Agonists bind to the extracellular domain and activate Gq/11-mediated signaling, leading to phospholipase C activation, inositol trisphosphate (IP3) generation, calcium release, and downstream cellular responses[7][1]

03

Biological functions

Signal transductionG protein-coupled UTP receptor activityRegulation of phospholipase C activationModulation of inositol phosphate and calcium signalingERK1/2 activation
04

Disease associations

CancerInflammationPotential roles in basal cell carcinomaDesmoid diseaseHereditaryOther
05

Safety considerations

No major clinical drug programs targeting P2Y4 specificallypotential safety issues might include altered calcium signaling and effects on epithelial or neuronal function due to broad pathway involvement[7][2]
06

Interacting drugs

UTP (agonist)

3 more in the full profile.

07

Biomarkers

None established for patient selectionexpression levels may be monitored in research or in disease states linked to receptor pathway[1][7]

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