EGFRvIII and DNA double-strand break repair: a molecular mechanism for radioresistance in glioblastoma

Cancer Res. 2009 May 15;69(10):4252-9. doi: 10.1158/0008-5472.CAN-08-4853. Epub 2009 May 12.

Abstract

Glioblastoma multiforme (GBM) is the most lethal of brain tumors and is highly resistant to ionizing radiation (IR) and chemotherapy. Here, we report on a molecular mechanism by which a key glioma-specific mutation, epidermal growth factor receptor variant III (EGFRvIII), confers radiation resistance. Using Ink4a/Arf-deficient primary mouse astrocytes, primary astrocytes immortalized by p53/Rb suppression, as well as human U87 glioma cells, we show that EGFRvIII expression enhances clonogenic survival following IR. This enhanced radioresistance is due to accelerated repair of DNA double-strand breaks (DSB), the most lethal lesion inflicted by IR. The EGFR inhibitor gefitinib (Iressa) and the phosphatidylinositol 3-kinase (PI3K) inhibitor LY294002 attenuate the rate of DSB repair. Importantly, expression of constitutively active, myristylated Akt-1 accelerates repair, implicating the PI3K/Akt-1 pathway in radioresistance. Most notably, EGFRvIII-expressing U87 glioma cells show elevated activation of a key DSB repair enzyme, DNA-dependent protein kinase catalytic subunit (DNA-PKcs). Enhanced radioresistance is abrogated by the DNA-PKcs-specific inhibitor NU7026, and EGFRvIII fails to confer radioresistance in DNA-PKcs-deficient cells. In vivo, orthotopic U87-EGFRvIII-derived tumors display faster rates of DSB repair following whole-brain radiotherapy compared with U87-derived tumors. Consequently, EGFRvIII-expressing tumors are radioresistant and continue to grow following whole-brain radiotherapy with little effect on overall survival. These in vitro and in vivo data support our hypothesis that EGFRvIII expression promotes DNA-PKcs activation and DSB repair, perhaps as a consequence of hyperactivated PI3K/Akt-1 signaling. Taken together, our results raise the possibility that EGFR and/or DNA-PKcs inhibition concurrent with radiation may be an effective therapeutic strategy for radiosensitizing high-grade gliomas.

Publication types

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

MeSH terms

  • Animals
  • Astrocytes / drug effects
  • Astrocytes / physiology
  • Astrocytes / radiation effects
  • Brain Neoplasms / drug therapy
  • Brain Neoplasms / genetics
  • Brain Neoplasms / mortality
  • Brain Neoplasms / pathology
  • Brain Neoplasms / radiotherapy
  • Cell Line, Tumor
  • Combined Modality Therapy
  • DNA Damage* / radiation effects
  • DNA Repair* / radiation effects
  • DNA, Neoplasm / genetics*
  • DNA, Neoplasm / radiation effects
  • Dacarbazine / analogs & derivatives
  • Dacarbazine / therapeutic use
  • Drug Resistance, Neoplasm
  • ErbB Receptors / genetics*
  • Fibroblasts / drug effects
  • Fibroblasts / physiology
  • Fibroblasts / radiation effects
  • Glioblastoma / drug therapy
  • Glioblastoma / genetics*
  • Glioblastoma / mortality
  • Glioblastoma / pathology
  • Glioblastoma / radiotherapy
  • Humans
  • Mice
  • Radiation, Ionizing
  • Survival Analysis
  • Survivors
  • Temozolomide

Substances

  • DNA, Neoplasm
  • epidermal growth factor receptor VIII
  • Dacarbazine
  • ErbB Receptors
  • Temozolomide