EGFRvIII upregulates DNA mismatch repair resulting in increased temozolomide sensitivity of MGMT promoter methylated glioblastoma

Oncogene. 2020 Apr;39(15):3041-3055. doi: 10.1038/s41388-020-1208-5. Epub 2020 Feb 17.

Abstract

The oncogene epidermal growth factor receptor variant III (EGFRvIII) is frequently expressed in glioblastomas (GBM) but its impact on therapy response is still under controversial debate. Here we wanted to test if EGFRvIII influences the sensitivity towards the alkylating agent temozolomide (TMZ). Therefore, we retrospectively analyzed the survival of 336 GBM patients, demonstrating that under standard treatment, which includes TMZ, EGFRvIII expression is associated with prolonged survival, but only in patients with O6-methylguanine-DNA methyltransferase (MGMT) promoter methylated tumors. Using isogenic GBM cell lines with endogenous EGFRvIII expression we could demonstrate that EGFRvIII increases TMZ sensitivity and results in enhanced numbers of DNA double-strand breaks and a pronounced S/G2-phase arrest after TMZ treatment. We observed a higher expression of DNA mismatch repair (MMR) proteins in EGFRvIII+ cells and patient tumor samples, which was most pronounced for MSH2 and MSH6. EGFRvIII-specific knockdown reduced MMR protein expression thereby increasing TMZ resistance. Subsequent functional kinome profiling revealed an increased activation of p38- and ERK1/2-dependent signaling in EGFRvIII expressing cells, which regulates MMR protein expression downstream of EGFRvIII. In summary, our results demonstrate that the oncoprotein EGFRvIII sensitizes a fraction of GBM to current standard of care treatment through the upregulation of DNA MMR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain Neoplasms / genetics
  • Brain Neoplasms / mortality
  • Brain Neoplasms / therapy*
  • Cell Line, Tumor
  • Chemoradiotherapy / methods
  • Cohort Studies
  • DNA Methylation
  • DNA Mismatch Repair / drug effects
  • DNA Mismatch Repair / genetics
  • DNA Modification Methylases / genetics*
  • DNA Modification Methylases / metabolism
  • DNA Repair Enzymes / genetics*
  • DNA Repair Enzymes / metabolism
  • DNA-Binding Proteins / genetics
  • Drug Resistance, Neoplasm / genetics*
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism
  • Female
  • Gene Expression Regulation, Neoplastic
  • Gene Knockdown Techniques
  • Glioblastoma / genetics
  • Glioblastoma / mortality
  • Glioblastoma / therapy*
  • Humans
  • Kaplan-Meier Estimate
  • MAP Kinase Signaling System / genetics
  • Mice
  • MutS Homolog 2 Protein / genetics
  • Mutation
  • Promoter Regions, Genetic / genetics
  • Retrospective Studies
  • Temozolomide / pharmacology*
  • Temozolomide / therapeutic use
  • Tumor Suppressor Proteins / genetics*
  • Tumor Suppressor Proteins / metabolism
  • Up-Regulation
  • Xenograft Model Antitumor Assays

Substances

  • DNA-Binding Proteins
  • G-T mismatch-binding protein
  • Tumor Suppressor Proteins
  • DNA Modification Methylases
  • MGMT protein, human
  • EGFR protein, human
  • ErbB Receptors
  • MSH2 protein, human
  • MutS Homolog 2 Protein
  • DNA Repair Enzymes
  • Temozolomide