A preclinical study demonstrating the efficacy of nilotinib in inhibiting the growth of pediatric high-grade glioma

J Neurooncol. 2015 May;122(3):471-80. doi: 10.1007/s11060-015-1744-y. Epub 2015 Mar 4.

Abstract

Solid tumors arising from malignant transformation of glial cells are one of the leading causes of central nervous system tumor-related death in children. Recurrence in spite of rigorous surgical and chemoradiation therapies remains a major hurdle in management of these tumors. Here, we investigate the efficacy of the second-generation receptor tyrosine kinase inhibitor nilotinib as a therapeutic option for the management of pediatric gliomas. We have utilized two independent pediatric high-grade glioma cell lines with either high platelet-derived growth factor receptor alpha (PDGFRα) or high PDGFRβ expression in in vitro assays to investigate the specific downstream effects of nilotinib treatment. Using in vitro cell-based assays we show that nilotinib inhibits PDGF-BB-dependent activation of PDGFRα. We further show that nilotinib is able to decrease cell proliferation and anchorage-independent growth via suppression of AKT and ERK1/2 signaling pathways. Our results suggest that nilotinib may be effective for management of a PDGFRα-dependent group of pediatric gliomas.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Becaplermin
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Colony-Forming Units Assay
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Gene Expression Regulation, Neoplastic / drug effects*
  • Glioma / drug therapy
  • Glioma / pathology*
  • Humans
  • MAP Kinase Signaling System / drug effects
  • Mice
  • Mice, SCID
  • Oncogene Protein v-akt / metabolism
  • Proto-Oncogene Proteins c-sis / metabolism
  • Pyrimidines / pharmacology*
  • Pyrimidines / therapeutic use
  • Receptor, Platelet-Derived Growth Factor alpha / metabolism
  • Time Factors
  • Vinculin / metabolism
  • Xenograft Model Antitumor Assays

Substances

  • Enzyme Inhibitors
  • Proto-Oncogene Proteins c-sis
  • Pyrimidines
  • Vinculin
  • Becaplermin
  • Receptor, Platelet-Derived Growth Factor alpha
  • Oncogene Protein v-akt
  • nilotinib