Imatinib mesylate inhibits the profibrogenic activity of TGF-beta and prevents bleomycin-mediated lung fibrosis

J Clin Invest. 2004 Nov;114(9):1308-16. doi: 10.1172/JCI19603.

Abstract

Idiopathic pulmonary fibrosis is a progressive and fatal fibrotic disease of the lungs with unclear etiology. Prior efforts to treat idiopathic pulmonary fibrosis that focused on anti-inflammatory therapy have not proven to be effective. Recent insight suggests that the pathogenesis is mediated through foci of dysregulated fibroblasts driven by profibrotic cytokine signaling. TGF-beta and PDGF are 2 of the most potent of these cytokines. In the current study, we investigated the role of TGF-beta-induced fibrosis mediated by activation of the Abelson (Abl) tyrosine kinase. Our data indicate that fibroblasts respond to TGF-beta by stimulating c-Abl kinase activity independently of Smad2/3 phosphorylation or PDGFR activation. Moreover, inhibition of c-Abl by imatinib prevented TGF-beta-induced ECM gene expression, morphologic transformation, and cell proliferation independently of any effect on Smad signaling. Further, using a mouse model of bleomycin-induced pulmonary fibrosis, we found a significant inhibition of lung fibrosis by imatinib. Thus, Abl family members represent common targets for the modulation of profibrotic cytokine signaling.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Benzamides
  • Bleomycin / adverse effects*
  • Bleomycin / pharmacology
  • Blotting, Western
  • Cell Proliferation
  • Cells, Cultured
  • Collagen / metabolism
  • Cytokines / metabolism
  • Fibroblasts / cytology
  • Fibroblasts / metabolism
  • Fibronectins / metabolism
  • Fibrosis
  • Imatinib Mesylate
  • Immunoprecipitation
  • Inflammation
  • Luciferases / metabolism
  • Lung / cytology
  • Lung / drug effects
  • Lung / pathology*
  • Mice
  • Mice, Knockout
  • NIH 3T3 Cells
  • Piperazines / pharmacology*
  • Proto-Oncogene Proteins c-abl / metabolism
  • Pyrimidines / pharmacology*
  • Receptors, Platelet-Derived Growth Factor / metabolism
  • Signal Transduction
  • Time Factors
  • Transforming Growth Factor beta / metabolism*
  • Transforming Growth Factor beta2
  • Transgenes

Substances

  • Antineoplastic Agents
  • Benzamides
  • Cytokines
  • Fibronectins
  • Piperazines
  • Pyrimidines
  • Transforming Growth Factor beta
  • Transforming Growth Factor beta2
  • Bleomycin
  • Imatinib Mesylate
  • Collagen
  • Luciferases
  • Receptors, Platelet-Derived Growth Factor
  • Proto-Oncogene Proteins c-abl