Imatinib mesylate inhibits platelet derived growth factor stimulated proliferation of rheumatoid synovial fibroblasts

Biochem Biophys Res Commun. 2006 Aug 18;347(1):31-5. doi: 10.1016/j.bbrc.2006.06.052. Epub 2006 Jun 21.

Abstract

Synovial fibroblast is the key cell type in the growth of the pathological synovial tissue in arthritis. Here, we show that platelet-derived growth factor (PDGF) is a potent mitogen for synovial fibroblasts isolated from patients with rheumatoid arthritis. Inhibition of PDGF-receptor signalling by imatinib mesylate (1muM) completely abrogated the PDGF-stimulated proliferation and inhibited approximately 70% of serum-stimulated proliferation of synovial fibroblasts. Similar extent of inhibition was observed when PDGF was neutralized with anti-PDGF antibodies, suggesting that imatinib mesylate does not inhibit pathways other than those mediated by PDGF-receptors. No signs of apoptosis were detected in synovial fibroblasts cultured in the presence of imatinib. These results suggest that imatinib mesylate specifically inhibits PDGF-stimulated proliferation of synovial fibroblasts, and that inhibition of PDGF-receptors could represent a feasible target for novel antirheumatic therapies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arthritis, Rheumatoid / pathology*
  • Arthritis, Rheumatoid / physiopathology
  • Benzamides
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Drug Combinations
  • Fibroblasts / drug effects*
  • Fibroblasts / pathology*
  • Humans
  • Imatinib Mesylate
  • Piperazines / administration & dosage*
  • Platelet-Derived Growth Factor / administration & dosage*
  • Protein Kinase Inhibitors / administration & dosage
  • Pyrimidines / administration & dosage*
  • Synovial Membrane / drug effects
  • Synovial Membrane / pathology*

Substances

  • Benzamides
  • Drug Combinations
  • Piperazines
  • Platelet-Derived Growth Factor
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Imatinib Mesylate