Platelet P2Y₁ receptor exhibits constitutive G protein signaling and β-arrestin 2 recruitment.

ABSTRACT:

Background

Purinergic P2Y₁ and P2Y₁₂ receptors (P2Y₁-R and P2Y₁₂-R) are G protein-coupled receptors (GPCR) activated by adenosine diphosphate (ADP) to mediate platelet activation, thereby playing a pivotal role in hemostasis and thrombosis. While P2Y₁₂-R is the major target of antiplatelet drugs, no P2Y₁-R antagonist has yet been developed for clinical use. However, accumulating data suggest that P2Y₁-R inhibition would ensure efficient platelet inhibition with minimal effects on bleeding. In this context, an accurate characterization of P2Y₁-R antagonists constitutes an important preliminary step.

Results

Here, we investigated the pharmacology of P2Y₁-R signaling through Gq an

SUBMITTER: Ribes A 

PROVIDER: S-EPMC9890698 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature