P2RY12
Description
The P2RY12 (purinergic receptor P2Y12) is a protein-coding gene located on chromosome 3.
P2RY12 is a G protein-coupled receptor (GPCR) that belongs to the Gi class and functions as a chemoreceptor for adenosine diphosphate (ADP). It's part of the P2Y receptor family, which includes several subtypes with varying pharmacological selectivity for adenosine and uridine nucleotides. P2RY12 is crucial for platelet aggregation, making it a target for treating thromboembolisms and other clotting disorders. Two transcript variants, encoding the same isoform, have been identified for this gene.
This receptor is found primarily on blood platelets but also in other peripheral tissues, playing a key role in blood clotting. In the central nervous system, P2RY12 is exclusively expressed on microglia. It regulates physiological and pathological microglial functions, such as monitoring neuronal activity and providing neuroprotection.
Several drugs, including clopidogrel (Plavix), prasugrel (Efient, Effient), ticagrelor (Brilinta), and cangrelor (Kengreal), are marketed as antiplatelet agents that bind to P2RY12. These drugs are commonly used in combination with aspirin, referred to as dual antiplatelet therapy, as a first-line treatment for acute coronary syndrome. A 2019 randomized trial suggested that prasugrel might be more effective than ticagrelor.
For patients undergoing percutaneous coronary intervention (PCI) for an ST-segment elevation myocardial infarction (STEMI), US, European, and Canadian guidelines recommend administering a P2Y12 inhibitor as soon as possible. However, it remains unclear whether administering these medications before hospital arrival provides additional benefits compared to in-hospital administration.
P2RY12 acts as a receptor for ADP and ATP, coupling with G-proteins to inhibit the adenylyl cyclase second messenger system. It is not activated by UDP or UTP. This receptor is essential for normal platelet aggregation and blood coagulation. This function is supported by a range of studies, including those found in PubMed IDs: 11104774, 11196645, 11502873, 12578987, 24670650, and 24784220.
P2RY12 is also known as ADPG-R, BDPLT8, HORK3, P2T(AC), P2Y(12)R, P2Y(AC), P2Y(ADP), P2Y(cyc), P2Y12, SP1999.
