Target intelligence / Profile preview

P2Y purinoceptor family (P2Y receptors) (P2Y receptors)

Target
P2Y receptors
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The P2Y purinoceptor family consists of eight human G protein-coupled receptors (P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, and P2Y14) that are activated by extracellular nucleotides such as ATP, ADP, UTP, and UDP (Burnstock, 2018, Purinergic Signalling). These receptors are broadly expressed across various tissues and play critical roles in physiological processes including platelet aggregation, vascular tone regulation, inflammatory responses, and neurotransmission (Abbracchio et al., 2006, Pharmacological Reviews). The family is structurally and functionally divided into two subgroups: the Gq-coupled receptors (P2Y1, 2, 4, 6, 11) which activate phospholipase C, and the Gi-coupled receptors (P2Y12, 13, 14) which inhibit adenylyl cyclase. Clinically, the P2Y12 receptor is a major target for antiplatelet drugs like clopidogrel and ticagrelor, which are essential in managing acute coronary syndromes and preventing stent thrombosis (Capodanno et al., 2019, Nature Reviews Cardiology). Other members, such as P2Y2, are targeted for conditions like dry eye syndrome using agonists like diquafosol to stimulate tear secretion (Lau et al., 2014, Expert Opinion on Investigational Drugs). Ongoing research continues to explore the therapeutic potential of this family in treating chronic pain, neurodegeneration, and cancer.

Other names
Purinergic P2Y receptorsP2Y purinoceptorsP2Y receptor familyNucleotide-activated G protein-coupled receptors
02

Mechanism of action

Antagonism of P2Y12 receptors to inhibit ADP-induced platelet aggregation; Agonism of P2Y2 receptors to stimulate chloride and water secretion in epithelial cells.

03

Biological functions

Signal transductionPlatelet aggregationInflammationVasodilationNeurotransmissionIon transportMucin secretion
04

Disease associations

Cardiovascular diseaseThrombosisInflammationDry eye syndromePainCancerAsthma
05

Safety considerations

Increased risk of bleedingDyspneaBradycardiaGastrointestinal irritationNeutropenia (rare, with older thienopyridines)
06

Interacting drugs

Clopidogrel

6 more in the full profile.

07

Biomarkers

Platelet reactivity index (PRI)VASP-phosphorylation assayADP-induced platelet aggregation

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