Dual P2Y 12 receptor signaling in thrombin-stimulated platelets--involvement of phosphoinositide 3-kinase beta but not gamma isoform in Ca2+ mobilization and procoagulant activity

FEBS J. 2008 Jan;275(2):371-85. doi: 10.1111/j.1742-4658.2007.06207.x. Epub 2007 Dec 13.

Abstract

During thrombus formation, thrombin, which is abundantly present at sites of vascular injury, activates platelets in part via autocrine-produced ADP. We investigated the signaling pathways by which thrombin and ADP in synergy induced platelet Ca(2+) elevation and procoagulant activity, and we monitored the consequences for the coagulation process. Even at high thrombin concentration, autocrine and added ADP enhanced and prolonged Ca(2+) depletion from internal stores via stimulation of the P2Y(12) receptors. This P2Y(12)-dependent effect was mediated via two distinct signaling pathways. The first is enhanced Ca(2+) mobilization by the inositol 1,4,5-trisphosphate receptors due to inhibition of protein kinase A. The second pathway concerns prolonged activation of phosphoinositide 3-kinase (PI3-K) and phospholipase C. Experiments with phosphoinositide 3-kinase isoform-selective inhibitors and p110gamma deficient platelets demonstrated that the phosphoinositide 3-kinase beta and not the phosphoinositide 3-kinase gamma isoform is responsible for the prolonged Ca(2+) response and for the subsequent increases in procoagulant activity and coagulation. Taken together, these results demonstrate a dual P2Y(12)-dependent signaling mechanism, which increases the platelet-activating effect of thrombin by prolongation of Ca(2+) elevation, thereby facilitating the coagulation process.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Blood Platelets / drug effects*
  • Blood Platelets / enzymology
  • Blood Platelets / metabolism
  • Calcium / metabolism*
  • Coagulants / pharmacology*
  • Cyclic AMP-Dependent Protein Kinases / metabolism
  • Flow Cytometry
  • Humans
  • In Vitro Techniques
  • Inositol 1,4,5-Trisphosphate Receptors / metabolism
  • Isoenzymes / metabolism*
  • Phosphatidylinositol 3-Kinases / metabolism*
  • Receptors, Purinergic P2 / metabolism*
  • Receptors, Purinergic P2Y12
  • Signal Transduction*
  • Thrombin / pharmacology*

Substances

  • Coagulants
  • Inositol 1,4,5-Trisphosphate Receptors
  • Isoenzymes
  • P2RY12 protein, human
  • Receptors, Purinergic P2
  • Receptors, Purinergic P2Y12
  • Phosphatidylinositol 3-Kinases
  • Cyclic AMP-Dependent Protein Kinases
  • Thrombin
  • Calcium