P2Y purinoceptor 12 (P2Y12) (P2Y12)

The P2Y purinoceptor 12 (P2Y12) is a G protein-coupled receptor primarily expressed on the surface of platelets, where it plays a central role in blood clotting and thrombus formation (UniProt Q9H244). It is activated by adenosine diphosphate (ADP), which is released from platelet storage granules upon initial activation. Once activated, P2Y12 couples with Gi proteins to inhibit adenylyl cyclase and activate phosphoinositide 3-kinase (PI3K) pathways, leading to sustained platelet aggregation and stabilization of the thrombus (PubMed: 11173810). Because of its critical role in arterial thrombosis, P2Y12 is a major therapeutic target for antiplatelet therapy in patients with cardiovascular diseases such as acute coronary syndrome or those undergoing percutaneous coronary intervention (StatPearls: NBK538152). Drugs targeting this receptor, including thienopyridines like clopidogrel and non-thienopyridines like ticagrelor, work by blocking ADP binding, thereby preventing excessive clot formation. However, the primary clinical challenge associated with P2Y12 inhibition is the increased risk of bleeding, requiring a careful balance between antithrombotic efficacy and safety (PubMed: 25154541).

Other names

P2Y12 receptorADP receptorP2RY12P2T(AC)P2Y(ADP)P2Y(AC)HMPL-1SP1999

P2Y12 receptor antagonism