Target intelligence / Profile preview

P2Y purinoceptor 12 (P2Y12)

Target
P2Y12
Molecular classification
G protein-coupled receptor, Purinergic receptor
01

Overview

The P2Y12 receptor is a G protein-coupled purinergic receptor primarily activated by adenosine diphosphate (ADP). It plays a critical role in platelet aggregation and is a key target for antithrombotic therapies. It is predominantly expressed on platelets, where it mediates ADP-induced platelet activation, and in the central nervous system, exclusively on microglia where it mediates neuroprotection. Pharmacological inhibition of P2Y12 leads to impaired platelet aggregation and is used to prevent thrombotic events.

Other names
ADP receptorP2RY12
02

Mechanism of action

P2Y12 receptor antagonists inhibit ADP-induced platelet activation and aggregation by blocking the binding of ADP to the P2Y12 receptor, which reduces adenylyl cyclase activity, leading to decreased cAMP levels and ultimately reduced platelet activation.

03

Biological functions

Platelet aggregationInflammationMicroglial activationSignal transduction
04

Disease associations

Thrombotic disordersCardiovascular diseaseInflammationAsthmaCancer
05

Safety considerations

BleedingThrombocytopenic purpura (TTP)
06

Interacting drugs

Clopidogrel

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