Cyclic AMP-insensitive activation of c-Src and Syk protein-tyrosine kinases through platelet membrane glycoprotein VI

J Biol Chem. 1995 Nov 24;270(47):28029-36. doi: 10.1074/jbc.270.47.28029.

Abstract

Platelet glycoprotein (GP) VI is a so-far uncharacterized 62-kDa membrane protein, whose deficiency results in selective impairment in collagen-induced platelet aggregation. Our group previously reported a human polyclonal antibody (anti-p62 IgG) that induces activation of normal, but not of GPVI-deficient, platelets in an Fc-independent manner. The F(ab')2 fragments of this antibody (F(ab')2-anti-p62) stimulated tyrosine phosphorylation of numerous proteins, which was not prevented even in the presence of cAMP-increasing agents such as prostacyclin. Pretreatment of platelets with the protein-tyrosine kinase (PTK) inhibitor tyrphostin A47 completely abolished F(ab')2-anti-p62-induced platelet aggregation in parallel with dose-dependent inhibition of protein-tyrosine phosphorylation, indicating an essential requirement of PTK activity for generating GPVI-mediated signaling. We found that two cytosolic PTKs, c-Src and Syk, became rapidly activated in response to F(ab')2-anti-p62 in a way insensitive to elevation of cAMP. In contrast, in the presence of prostacyclin, F(ab')2-anti-p62 did not stimulate tyrosine phosphorylation of the focal adhesion kinase. cAMP-insensitive activation of c-Src and Syk was also observed in collagen but not thrombin-stimulated platelets. Moreover, either F(ab')2-anti-p62 or collagen stimulated cAMP-insensitive tyrosine phosphorylation of phospholipase C-gamma 2. These results indicate that the receptor-mediated activation of several PTKs in platelets is regulated through a cAMP-sensitive or -insensitive mechanism depending on the nature of each stimulus, and also suggest that GPVI engagement is coupled to cAMP-insensitive activation of c-Src and Syk accompanied by tyrosine phosphorylation of numerous substrates including phospholipase C-gamma 2 in a manner similar to collagen stimulation.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Blood Platelets / drug effects
  • Blood Platelets / physiology*
  • Caffeic Acids / pharmacology
  • Collagen / pharmacology
  • Cyclic AMP / physiology*
  • Cytosol / enzymology
  • Enzyme Precursors / blood*
  • Epoprostenol / pharmacology
  • Humans
  • Immunoglobulin Fab Fragments / pharmacology
  • Immunoglobulin G / blood
  • Intracellular Signaling Peptides and Proteins
  • Isoenzymes / blood
  • Kinetics
  • Oligopeptides / pharmacology
  • Phosphorylation
  • Phosphotyrosine / metabolism
  • Platelet Aggregation Inhibitors / pharmacology
  • Platelet Membrane Glycoproteins / deficiency
  • Platelet Membrane Glycoproteins / physiology*
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Protein-Tyrosine Kinases / blood*
  • Proto-Oncogene Proteins pp60(c-src) / blood*
  • Reference Values
  • Signal Transduction
  • Syk Kinase
  • Thrombasthenia / blood
  • Thrombin / pharmacology
  • Type C Phospholipases / blood
  • Tyrphostins*

Substances

  • Caffeic Acids
  • Enzyme Precursors
  • Immunoglobulin Fab Fragments
  • Immunoglobulin G
  • Intracellular Signaling Peptides and Proteins
  • Isoenzymes
  • Oligopeptides
  • Platelet Aggregation Inhibitors
  • Platelet Membrane Glycoproteins
  • Tyrphostins
  • tyrphostin 47
  • Phosphotyrosine
  • Collagen
  • arginyl-glycyl-aspartyl-serine
  • Epoprostenol
  • Cyclic AMP
  • Protein-Tyrosine Kinases
  • Proto-Oncogene Proteins pp60(c-src)
  • SYK protein, human
  • Syk Kinase
  • Type C Phospholipases
  • Thrombin