STAT3 Serine 727 Phosphorylation: A Relevant Target to Radiosensitize Human Glioblastoma

Brain Pathol. 2016 Jan;26(1):18-30. doi: 10.1111/bpa.12254. Epub 2015 Apr 30.

Abstract

Radiotherapy is an essential component of glioma standard treatment. Glioblastomas (GBM), however, display an important radioresistance leading to tumor recurrence. To improve patient prognosis, there is a need to radiosensitize GBM cells and to circumvent the mechanisms of resistance caused by interactions between tumor cells and their microenvironment. STAT3 has been identified as a therapeutic target in glioma because of its involvement in mechanisms sustaining tumor escape to both standard treatment and immune control. Here, we studied the role of STAT3 activation on tyrosine 705 (Y705) and serine 727 (S727) in glioma radioresistance. This study explored STAT3 phosphorylation on Y705 (pSTAT3-Y705) and S727 (pSTAT3-S727) in glioma cell lines and in clinical samples. Radiosensitizing effect of STAT3 activation down-modulation by Gö6976 was explored. In a panel of 15 human glioma cell lines, we found that the level of pSTAT3-S727 was correlated to intrinsic radioresistance. Moreover, treating GBM cells with Gö6976 resulted in a highly significant radiosensitization associated to a concomitant pSTAT3-S727 down-modulation only in GBM cell lines that exhibited no or weak pSTAT3-Y705. We report the constitutive activation of STAT3-S727 in all GBM clinical samples. Targeting pSTAT3-S727 mainly in pSTAT3-Y705-negative GBM could be a relevant approach to improve radiation therapy.

Keywords: Gö6976; STAT3; glioma; radiotherapy; resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Brain Neoplasms / drug therapy
  • Brain Neoplasms / metabolism*
  • Brain Neoplasms / radiotherapy*
  • Carbazoles / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Proliferation / radiation effects
  • Colony-Forming Units Assay
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology
  • Gene Expression Regulation, Neoplastic / drug effects
  • Gene Expression Regulation, Neoplastic / radiation effects
  • Glioblastoma / drug therapy
  • Glioblastoma / metabolism*
  • Glioblastoma / pathology*
  • Glioblastoma / radiotherapy
  • Humans
  • Phosphorylation / drug effects
  • Phosphorylation / radiation effects
  • Radiation
  • Radiation Tolerance / drug effects
  • Radiation Tolerance / radiation effects
  • STAT3 Transcription Factor / metabolism*
  • Serine / metabolism*
  • Signal Transduction / drug effects
  • Signal Transduction / radiation effects
  • Spectrophotometry
  • Statistics, Nonparametric
  • Time Factors
  • X-Rays

Substances

  • Carbazoles
  • Enzyme Inhibitors
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • Go 6976
  • Serine