Antithrombotic effects of targeting alphaIIbbeta3 signaling in platelets

Blood. 2009 Apr 9;113(15):3585-92. doi: 10.1182/blood-2008-09-180687. Epub 2008 Nov 12.

Abstract

alphaIIbbeta3 interaction with fibrinogen promotes Src-dependent platelet spreading in vitro. To determine the consequences of this outside-in signaling pathway in vivo, a "beta3(Delta760-762)" knockin mouse was generated that lacked the 3 C-terminal beta3 residues (arginine-glycine-threonine [RGT]) necessary for alphaIIbbeta3 interaction with c-Src, but retained beta3 residues necessary for talin-dependent fibrinogen binding. beta3(Delta760-762) mice were compared with wild-type beta3(+/+) littermates, beta3(+/-) heterozygotes, and knockin mice where beta3 RGT was replaced by beta1 C-terminal cysteine-glycine-lysine (EGK) to potentially enable signaling by Src kinases other than c-Src. Whereas beta3(+/+), beta3(+/-) and beta3/beta1(EGK) platelets spread and underwent tyrosine phosphorylation normally on fibrinogen, beta3(Delta760-762) platelets spread poorly and exhibited reduced tyrosine phosphorylation of c-Src substrates, including beta3 (Tyr(747)). Unlike control mice, beta3(Delta760-762) mice were protected from carotid artery thrombosis after vessel injury with FeCl(3). Some beta3(Delta760-762) mice exhibited prolonged tail bleeding times; however, none demonstrated spontaneous bleeding, excess bleeding after surgery, fecal blood loss, or anemia. Fibrinogen binding to beta3(Delta760-762) platelets was normal in response to saturating concentrations of protease-activated receptor 4 or glycoprotein VI agonists, but responses to adenosine diphosphate were impaired. Thus, deletion of beta3 RGT disrupts c-Src-mediated alphaIIbbeta3 signaling and confers protection from arterial thrombosis. Consequently, targeting alphaIIbbeta3 signaling may represent a feasible antithrombotic strategy.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Blood Platelets / physiology*
  • Fibrinogen / metabolism
  • Gene Knock-In Techniques
  • Hemorrhage / prevention & control
  • Hemostasis / physiology
  • Mice
  • Mice, Mutant Strains
  • Platelet Glycoprotein GPIIb-IIIa Complex / chemistry
  • Platelet Glycoprotein GPIIb-IIIa Complex / genetics*
  • Platelet Glycoprotein GPIIb-IIIa Complex / metabolism*
  • Protein Structure, Tertiary
  • Signal Transduction / physiology*
  • Thrombosis / metabolism
  • Thrombosis / physiopathology
  • Thrombosis / prevention & control*
  • src-Family Kinases / metabolism

Substances

  • Platelet Glycoprotein GPIIb-IIIa Complex
  • Fibrinogen
  • src-Family Kinases