Phosphoinositide 3-kinase inhibition reverses platelet aggregation triggered by the combination of the neutrophil proteinases elastase and cathepsin G without impairing alpha(IIb)beta(3) integrin activation

FEBS Lett. 2000 Nov 10;484(3):184-8. doi: 10.1016/s0014-5793(00)02152-9.

Abstract

Neutrophil elastase (NE) upregulates the fibrinogen binding activity of the platelet integrin alpha(IIb)beta(3) through proteolysis of the alpha(IIb) subunit. This cleavage allows a strong potentiation of platelet aggregation induced by low concentrations of cathepsin G (CG), another neutrophil serine proteinase. During this activation process, we observed a strong fibrinogen binding and aggregation-dependent phosphatidylinositol 3,4-bis-phosphate (PtdIns(3,4)P(2)) accumulation. PtdIns(3,4)P(2) has been suggested to play a role in the stabilization of platelet aggregation, possibly through the control of a maintained alpha(IIb)beta(3) integrin activation. Here we show that inhibition of phosphoinositide 3-kinase (PI 3-K) by very low concentrations of wortmannin or LY294002 transformed the irreversible platelet aggregation induced by a combination of NE and low concentrations of CG into a reversible aggregation. However, although inhibition of PI 3-K was very efficient in inducing platelet disaggregation, it did not modify the level of alpha(IIb)beta(3) activation as assessed by binding of an activation-dependent antibody. These results indicate that PI 3-K activity can control the irreversibility of platelet aggregation even under conditions where alpha(IIb)beta(3) integrin remains activated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androstadienes / pharmacology
  • Blood Platelets / drug effects
  • Blood Platelets / physiology*
  • Cathepsin G
  • Cathepsins / pharmacology
  • Cathepsins / physiology*
  • Chromones / pharmacology
  • Enzyme Inhibitors / pharmacology*
  • Fibrinogen / metabolism
  • Humans
  • In Vitro Techniques
  • Leukocyte Elastase / pharmacology
  • Leukocyte Elastase / physiology*
  • Morpholines / pharmacology
  • Phosphatidylinositol 3-Kinases / blood*
  • Phosphatidylinositols / blood
  • Phosphoinositide-3 Kinase Inhibitors
  • Platelet Activation / physiology
  • Platelet Aggregation / drug effects
  • Platelet Aggregation / physiology*
  • Platelet Glycoprotein GPIIb-IIIa Complex / drug effects
  • Platelet Glycoprotein GPIIb-IIIa Complex / physiology*
  • Serine Endopeptidases
  • Wortmannin

Substances

  • Androstadienes
  • Chromones
  • Enzyme Inhibitors
  • Morpholines
  • Phosphatidylinositols
  • Phosphoinositide-3 Kinase Inhibitors
  • Platelet Glycoprotein GPIIb-IIIa Complex
  • 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
  • Fibrinogen
  • Cathepsins
  • Serine Endopeptidases
  • CTSG protein, human
  • Cathepsin G
  • Leukocyte Elastase
  • Wortmannin