Target intelligence / Profile preview

P2Y purinoceptor (P2Y receptor)

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

Overview

P2Y purinoceptors are a family of G protein-coupled receptors (GPCRs) that mediate cellular responses to extracellular nucleotides such as ATP, ADP, UTP, and UDP[1][6]. Unlike P2X receptors, which are ion channels, P2Y receptors transduce signals via G proteins leading to activation of second messenger pathways, primarily phospholipase C and sometimes adenylate cyclase, depending on the subtype[7][9]. Eight main human subtypes are characterized (P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, P2Y14), each with distinct ligand selectivity and tissue expression[7]. These receptors are critical in diverse physiological processes including platelet aggregation, immune modulation, inflammation, epithelial ion transport, and neuro-glial signaling[1][4][8]. Clinically, P2Y purinoceptors are key therapeutic targets, especially P2Y12 in antiplatelet therapy, while P2Y2 is being investigated as a novel target in inflammatory and autoimmune diseases[2][4][8].

Other names
P2Y receptorP2Y purinergic receptorP2Y nucleotide receptorP2Y GPCRP2Y family
02

Mechanism of action

Competitive antagonism of P2Y12 receptor (antiplatelet effect) Inhibition of ATP/UTP-activated signaling (anti-inflammatory effect) Blockade of ADP/UTP/UDP-induced G protein-coupled signal cascades Modulation of phospholipase C pathways Regulation of adenylate cyclase activity (for specific subtypes)

03

Biological functions

Signal transductionMediation of extracellular nucleotide signalingRegulation of immune responseModulation of cell proliferation and repairInflammatory response controlPlatelet aggregationRegulation of ion transport in epithelia
04

Disease associations

Cardiovascular diseaseInflammationNeurological diseases (e.g., epilepsy, neurodegeneration)Blood cell disorders (e.g., thrombosis)Autoimmune diseaseCystic fibrosisOther respiratory diseases (e.g., dry eye disease)
05

Safety considerations

Bleeding (with P2Y12 antagonists due to platelet inhibition)Immune suppression (potential with P2Y2 antagonists)On-target/off-target specificity (risk of broad physiological effects due to widespread receptor expression)
06

Interacting drugs

Clopidogrel (P2Y12 antagonist)

7 more in the full profile.

07

Biomarkers

Expression levels of P2Y receptor subtypes (e.g., P2Y12 in platelets as marker for antiplatelet therapy)Circulating nucleotide levelsInflammatory cytokine (e.g., IL-1β) induction of P2Y expression

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