Introduction of P2RY12
P2RY12, also known as purinergic receptor P2RY12, purinergic receptor P2Y12, purinergic receptor P2Y, P2Y(AC), P2Y(12)R, HORK3, BDPLT8, putative G-protein coupled receptor, G-protein coupled receptor SP1999, Gi-coupled ADP receptor HORK3, is a member of G-protein coupled receptors (GPCR) family, which has some receptor subtypes with different pharmacological selectivity. It is a 39.4 kDa molecule and in humans, encoded on the chromosome 3q25.1. Initially, the P2RY12 gene is reported that contains at least 2 exons, in charge of coding for 342 amino acid all length protein and separated by a 1,700 bp intron, localized upstream of the ATG codon. There are two transcript variants coding for the same isoform that have been identified for the P2RY12 gene.
|Basic Information of P2RY12|
|Protein Name||P2Y purinoceptor 12|
|Aliases||P2Y12, ADP-glucose receptor, ADPG-R, P2T(AC), P2Y(AC), P2Y(cyc), P2Y12 platelet ADP receptor, P2Y(ADP), SP1999|
|Organism||Homo sapiens (Human)|
Function of P2RY12 Membrane Protein
This receptor is found abundantly expressed in human platelets and smooth muscle, as well as spinal cords and numerous brain regions. It participates in the platelet aggregation and becomes a promising target for the clinical treatment of thromboembolism as well as other clotting disorders. Moreover, expressed sequence tags (ESTs) for P2RY12 have been isolated from B-cell, brain, eye, embryo, prostate, along with kidney and colon carcinoma libraries. Here, P2RY12, P2RY1, and P2X1 are three known ADP receptor subtypes on platelets. And ADP is secreted from red blood cells, damaged vessels, and platelets stimulated by other agonists. ADP can bind to P2RY1 to exert the platelet aggregation and to P2RY12, which amplifies the platelet aggregation. Furthermore, continued ADP-induced platelet aggregation demands the coactivation of both P2RY1 and P2RY12. P2RY12 receptor functions by inhibiting adenylyl cyclase through a Gi protein and enhances dense granule secretion, procoagulant activity, along with platelet aggregation. Without sustained activation of this receptor, aggregated platelets would disaggregate.
Fig.1 Structure of P2RY12 protein.
Application of P2RY12 Membrane Protein in Literature
The effect of more potent P2Y12 inhibitors in contrast to clopidogrel on efficacy as well as safety end points was consistent in younger and elderly patients. And data in this review implied that these P2Y12 inhibitors should not be withheld from eligible patients solely due to advanced age.
Proline played a critical role in P2Y12R ligand binding and signal defects and the homodimer formation of P2Y12R was important for the function and signaling of receptor. The new dominant negative variant confirmed the significant effect of R265 in EL3 in the P2Y12R functional integrity and suggested pathologic heterodimer formation might underlie this family bleeding phenotype.
Polymorphisms of the P2RY12 gene possibly predicted individual differences both in cancer and postoperative pain severity; this may be caused by functional alteration of nociceptive neurons via the neuron-glia interaction.
Short-term endurance training did not induce the downregulation of P2RY12 and upregulation of hsa-miR-223, while it had a positive influence on glycemic indices, platelet functions, physical fitness, together with body composition in female T2DM patients.
P2RY12 gene polymorphisms may correlate with higher risk of composite ischemic situations, stent thrombosis, unstable angina, and non-fatal myocardial infarction. However, there was no significant effect found on bleeding, mortality, and target vessel revascularization.
P2RY12 Preparation Options
To harvest an intact and functional target protein, we present a number of effective reconstitution formats and multiple active forms for membrane proteins. Our powerful Magic™ membrane protein production platform can guarantee a variety of flexible options such that customers can always find the most suitable match to meet their needs. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-P2RY12 antibody development services.
As a professional service provider with advanced platforms in the field of protein products, Creative Biolabs has obtained recognition from worldwide customers and scientists. Nowadays, we are pleased to launch and advertise our mature services of the membrane protein preparation in required forms by using multiple strategies. Please feel free to contact us for more information.