Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells

Anticancer Res. 2009 Jan;29(1):1-9.

Abstract

The ectopically expressed and deregulated fibroblast growth factor receptor 3 (FGFR3) has been observed in approximately 20% of multiple myeloma (MM) patients. In this study, we investigated whether the therapeutic effect of bortezomib is associated with FGFR3 expression.

Materials and methods: Cell proliferation and apoptosis assays were performed in minimal FGFR3 expressing U266 cells and compared to U266 cells overexpressing FGFR3 wild-type (T-U266), or Y373C (Y-U266) or K650E (K-U266) mutant FGFR3.

Results: Our results suggested cell survival decreases in a dose-dependent manner. Interestingly, expression of FGFR3 protein was similarly dose dependent on bortezomib. It is confirmed the bortezomib-induced apoptotic death is correlated with FGFR3 expression. Furthermore, increased expression of p-STAT3, Mcl-1 and VEGF suggested that bortezomib resistance associated with Y373C mutation and wild-type FGFR3 may be partly mediated through p-STAT3 signaling.

Conclusion: Our data indicates that Y373C mutation and wild-type FGFR3 may be associated with bortezomib-related treatment resistance in multiple myeloma.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Apoptosis / physiology
  • Boronic Acids / pharmacology*
  • Bortezomib
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Humans
  • Inhibitory Concentration 50
  • Multiple Myeloma / drug therapy*
  • Multiple Myeloma / enzymology*
  • Multiple Myeloma / genetics
  • Pyrazines / pharmacology*
  • Receptor, Fibroblast Growth Factor, Type 3 / biosynthesis*
  • Receptor, Fibroblast Growth Factor, Type 3 / deficiency
  • Receptor, Fibroblast Growth Factor, Type 3 / genetics
  • Receptor, Fibroblast Growth Factor, Type 3 / metabolism
  • STAT3 Transcription Factor / metabolism
  • Signal Transduction
  • Transfection

Substances

  • Antineoplastic Agents
  • Boronic Acids
  • Pyrazines
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • Bortezomib
  • FGFR3 protein, human
  • Receptor, Fibroblast Growth Factor, Type 3