Functional interaction between purinergic receptors: effect of ligands for A2Aand P2Y12receptors on P2Y1receptor function
Copyright policy )Functional interaction between purinergic receptors: effect of ligands for A2Aand P2Y12receptors on P2Y1receptor function
A(2A) adenosine receptor (A(2A)R), P2Y(1) receptor (P2Y(1)R) and P2Y(12) receptor (P2Y(12)R) are predominantly expressed on human platelets. The individual role of each of these receptors in platelet aggregation has been actively reported. Previously, hetero-oligomerization between these three receptors has been shown to occur. Here, we show that Ca(2+) signaling evoked by the P2Y(1)R agonist, 2-methylthioladenosine 5' diphosphate (2MeSADP) was significantly inhibited by the A(2A)R antagonist (ZM241385 (4-(2-[7-amino-2-(2-furyl)[1,2,4]-triazolo[2,3-α][1,3,5]triazin-5-yl amino]ethyl) phenol) and SCH442416) and the P2Y(12)R antagonist (ARC69931MX) (N6-(2-methyl-thioethyl)-2-(3,3,3-trifluoropropylthio)-β,γ-dichloromethylene-ATP)) using HEK293T cells expressing the three receptors. It was confirmed that inhibition of P2Y(1)R signaling by A(2A)R and P2Y(12)R antagonists was indeed mediated through A(2A)R and P2Y(12)R using 1321N1 human astrocytoma cells which do not express P2Y receptors. We expect that intermolecular signal transduction and specific conformational changes occur among components of hetero-oligomers formed by these three receptors.
- Waseda University Japan
- Tohoku University Japan
Receptor, Adenosine A2A, Triazines, Intracellular Space, Triazoles, Ligands, Receptors, Purinergic P2Y12, Adenosine A2 Receptor Antagonists, Receptors, Purinergic P2Y1, GPCR, HEK293 Cells, Gene Expression Regulation, Cell Line, Tumor, Purinergic P2Y Receptor Antagonists, Humans, Calcium Signaling, Purinergic P2Y Receptor Agonists, Protein Binding
Receptor, Adenosine A2A, Triazines, Intracellular Space, Triazoles, Ligands, Receptors, Purinergic P2Y12, Adenosine A2 Receptor Antagonists, Receptors, Purinergic P2Y1, GPCR, HEK293 Cells, Gene Expression Regulation, Cell Line, Tumor, Purinergic P2Y Receptor Antagonists, Humans, Calcium Signaling, Purinergic P2Y Receptor Agonists, Protein Binding
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