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P2Y12 receptors: structure and function.

M Cattaneo1

  • 1Dipartimento di Scienze della Salute, Università degli Studi di Milano, Unità di Medicina 3, Ospedale San Paolo, Milan, Italy.

Journal of Thrombosis and Haemostasis : JTH
|July 8, 2015
PubMed
Summary
This summary is machine-generated.

The platelet P2Y12 receptor (P2Y12R) is crucial for blood clotting and has roles in inflammation and cancer. New P2Y12R inhibitors show greater efficacy than clopidogrel in preventing cardiovascular events.

Keywords:
GTP‐binding proteinsP2Y12 purinoceptorP2Y12 purinoceptor antagonistsbleeding disorder due to P2RY12 defectinflammation

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Area of Science:

  • Pharmacology
  • Hematology
  • Immunology

Background:

  • The P2Y12 receptor (P2Y12R) for adenosine 5'diphosphate (ADP) is central to platelet function, hemostasis, and thrombosis.
  • Inherited P2Y12R defects cause bleeding disorders, and impaired platelet aggregation with ADP suggests P2Y12R dysfunction.
  • P2Y12R is implicated in allergic asthma pathogenesis and exhibits antitumor effects when inhibited or deficient.

Purpose of the Study:

  • To review the role of the P2Y12 receptor in platelet function, thrombosis, and other biological processes.
  • To discuss the clinical efficacy and limitations of P2Y12R antagonists, including clopidogrel, prasugrel, and ticagrelor.

Main Methods:

  • Literature review of studies on P2Y12 receptor function and pharmacology.
  • Analysis of clinical data comparing the efficacy of different P2Y12R inhibitors.

Main Results:

  • P2Y12R defects lead to bleeding diatheses and impaired platelet aggregation.
  • P2Y12R inhibition has antithrombotic, anti-inflammatory, and antitumor effects.
  • Newer P2Y12R antagonists (prasugrel, ticagrelor) are more effective than clopidogrel in preventing major adverse cardiovascular events in most patients.

Conclusions:

  • The P2Y12 receptor is a key target for antithrombotic therapy.
  • Prasugrel and ticagrelor offer improved P2Y12R inhibition and clinical outcomes compared to clopidogrel.
  • Further research into P2Y12R modulation may yield benefits beyond cardiovascular protection.