P2Y receptors are a family of purinergic G protein-coupled receptors, stimulated by nucleotides such as ATP, ADP, UTP, UDP and UDP-glucose.
To date, 8 P2Y receptors have been identified in humans: P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13 and P2Y14.
P2Y receptors are present in almost all human tissues.
P2Y receptors exert biological functions based on their G-protein coupling.
P2Y receptors mediate responses including vasodilation,blood clotting,and immune response.
The P2Y extracellular regions interact with the receptor ligands.
The intracellular regions activate the G protein,control receptor internalization, and mediate dimerization.
All P2Y receptors contain four extracellular cysteine residues which can form two disulfide bridges, which
are involved in ligand binding and signal transduction.
P2Y intracellular domains appear to be structurally and mechanistically similar to other GPCRs.
P2Y receptors respond to the presence of nucleotides in extracellular solution, either positively or negatively.
Nucleotides may be divided into two categories: purines and pyrimidines.
The activity of P2Y receptors is linked to regulation of the flow of Ca2+ and K+ ions by the receptor’s interactions with G proteins, modulating access to Ca2+ and K+ channels.
Changes in the concentration of Ca2+ help control regulation of cell metabolism, ATP production and the possibility of triggering apoptosis.
The most commonly prescribed drug targeting P2Y receptors is clopidogrel, an antiplatelet medication which acts on the P2Y12 receptor in a manner shared with other thienopyridines.
P2Y6 receptors have been shown to play a role in cerebral vasodilation.
P2Y11 is a regulator of immune response, and a common polymorphism carried by almost 20% of North European caucasians give increased risk of myocardial infarction.
The biological effects of P2Y receptor activation depends on how they couple to downstream signalling pathways of G proteins.
Human P2Y receptors have G protein coupling.