Time-resolved characterization of cAMP/PKA-dependent signaling reveals that platelet inhibition is a concerted process involving multiple signaling pathways

Blood. 2014 Jan 30;123(5):e1-e10. doi: 10.1182/blood-2013-07-512384. Epub 2013 Dec 9.

Abstract

One of the most important physiological platelet inhibitors is endothelium-derived prostacyclin which stimulates the platelet cyclic adenosine monophosphate/protein kinase A (cAMP/PKA)-signaling cascade and inhibits virtually all platelet-activating key mechanisms. Using quantitative mass spectrometry, we analyzed time-resolved phosphorylation patterns in human platelets after treatment with iloprost, a stable prostacyclin analog, for 0, 10, 30, and 60 seconds to characterize key mediators of platelet inhibition and activation in 3 independent biological replicates. We quantified over 2700 different phosphorylated peptides of which 360 were significantly regulated upon stimulation. This comprehensive and time-resolved analysis indicates that platelet inhibition is a multipronged process involving different kinases and phosphatases as well as many previously unanticipated proteins and pathways.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Blood Platelets / cytology
  • Blood Platelets / drug effects*
  • Cyclic AMP / metabolism
  • Cyclic AMP-Dependent Protein Kinases / metabolism*
  • Humans
  • Iloprost / pharmacology*
  • Phosphorylation / drug effects
  • Platelet Activation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology*
  • Protein Interaction Maps / drug effects
  • Signal Transduction / drug effects*

Substances

  • Platelet Aggregation Inhibitors
  • Cyclic AMP
  • Cyclic AMP-Dependent Protein Kinases
  • Iloprost