Fyn and SRC are effectors of oncogenic epidermal growth factor receptor signaling in glioblastoma patients

Cancer Res. 2009 Sep 1;69(17):6889-98. doi: 10.1158/0008-5472.CAN-09-0347. Epub 2009 Aug 18.

Abstract

Activating epidermal growth factor receptor (EGFR) mutations are common in many cancers including glioblastoma. However, clinical responses to EGFR inhibitors are infrequent and short-lived. We show that the Src family kinases (SFK) Fyn and Src are effectors of oncogenic EGFR signaling, enhancing invasion and tumor cell survival in vivo. Expression of a constitutively active EGFR mutant, EGFRvIII, resulted in activating phosphorylation and physical association with Src and Fyn, promoting tumor growth and motility. Gene silencing of Fyn and Src limited EGFR- and EGFRvIII-dependent tumor cell motility. The SFK inhibitor dasatinib inhibited invasion, promoted tumor regression, and induced apoptosis in vivo, significantly prolonging survival of an orthotopic glioblastoma model expressing endogenous EGFRvIII. Dasatinib enhanced the efficacy of an anti-EGFR monoclonal antibody (mAb 806) in vivo, further limiting tumor growth and extending survival. Examination of a large cohort of clinical samples showed frequent coactivation of EGFR and SFKs in glioblastoma patients. These results establish a mechanism linking EGFR signaling with Fyn and Src activation to promote tumor progression and invasion in vivo and provide rationale for combined anti-EGFR and anti-SFK targeted therapies.

Publication types

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

MeSH terms

  • Animals
  • Antibodies, Monoclonal / pharmacology
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Survival / drug effects
  • Central Nervous System Neoplasms / metabolism*
  • Central Nervous System Neoplasms / pathology
  • Dasatinib
  • Drug Synergism
  • Enzyme Activation
  • ErbB Receptors / antagonists & inhibitors
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism*
  • Gene Silencing
  • Glioblastoma / metabolism*
  • Glioblastoma / pathology
  • Humans
  • Mice
  • Mutation
  • Neoplasm Invasiveness
  • Neoplasm Transplantation
  • Phosphorylation
  • Protein Kinase Inhibitors / pharmacology
  • Proto-Oncogene Proteins c-fyn / metabolism*
  • Pyrimidines / pharmacology
  • Signal Transduction*
  • Thiazoles / pharmacology
  • src-Family Kinases / metabolism*

Substances

  • Antibodies, Monoclonal
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Thiazoles
  • epidermal growth factor receptor VIII
  • monoclonal antibody 806
  • ErbB Receptors
  • FYN protein, human
  • Proto-Oncogene Proteins c-fyn
  • src-Family Kinases
  • Dasatinib