Target intelligence / Profile preview

P2Y purinergic receptor family (P2Y receptor)

Target
P2Y receptor
Molecular classification
G protein-coupled receptor (GPCR), Receptor, Rhodopsin-like receptor subfamily
01

Overview

The P2Y purinergic receptor family consists of multiple subtypes of G protein-coupled receptors that bind extracellular nucleotides, triggering intracellular signaling cascades and modulating diverse physiological processes, including platelet aggregation, inflammation, cell proliferation, and muscle contraction. These receptors play key roles in cardiovascular health, immune responses, and some neurological and inflammatory diseases. Several subtypes serve as major drug targets for conditions like thrombosis and dry eye; however, drug development is challenged by limited ligand selectivity and risks related to bleeding or immune modulation.

Other names
P2Y receptor familyP2Y GPCRspurinergic P2Y receptorsmetabotropic P2 receptors
02

Mechanism of action

Agonism (activation of GPCR signaling, e.g., diquafosol at P2Y2); Antagonism (blocking platelet aggregation by inhibiting ADP binding at P2Y12, e.g., ticagrelor)

03

Biological functions

Signal transductionRegulation of intracellular calciumPlatelet aggregationRegulation of cAMPImmune responseInflammatory mediationSmooth muscle contraction
04

Disease associations

Cardiovascular disease (platelet aggregation, thrombosis)InflammationNeurological diseaseCancer (inflammatory and neural context)Cystic fibrosis (polymorphisms implicated)Bleeding disorders (mutations in P2Y12)
05

Safety considerations

Bleeding risk (with antiplatelet drugs targeting P2Y12)Excessive platelet inhibitionOff-target effects due to low drug selectivity
06

Interacting drugs

Diquafosol

5 more in the full profile.

07

Biomarkers

P2Y12 receptor gene polymorphisms (associated with platelet reactivity, arterial disease)P2Y2 polymorphisms in cystic fibrosis

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