A phosphoproteomic signature in endothelial cells predicts vascular toxicity of tyrosine kinase inhibitors used in CML

Blood Adv. 2018 Jul 24;2(14):1680-1684. doi: 10.1182/bloodadvances.2018020396.

Abstract

  1. Newer CML kinase inhibitors increase ischemia risk and are toxic to endothelial cells where they produce a proteomic toxicity signature.

  2. This phosphoproteomic EC toxicity signature predicts bosutinib to be safe, providing a potential screening tool for safer drug development.

Publication types

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

MeSH terms

  • Aniline Compounds / adverse effects*
  • Aniline Compounds / pharmacology
  • Human Umbilical Vein Endothelial Cells / metabolism*
  • Human Umbilical Vein Endothelial Cells / pathology
  • Humans
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
  • Nitriles / adverse effects*
  • Nitriles / pharmacology
  • Phosphoproteins / metabolism*
  • Protein Kinase Inhibitors / adverse effects*
  • Protein Kinase Inhibitors / pharmacology
  • Proteomics*
  • Quinolines / adverse effects*
  • Quinolines / pharmacology

Substances

  • Aniline Compounds
  • Nitriles
  • Phosphoproteins
  • Protein Kinase Inhibitors
  • Quinolines
  • bosutinib