Casein kinase 2 inhibition modulates the DNA damage response but fails to radiosensitize malignant glioma cells

Int J Oncol. 2012 Aug;41(2):776-82. doi: 10.3892/ijo.2012.1489. Epub 2012 May 18.

Abstract

Inhibitors of casein kinase 2 (CK2), a regulator of cell proliferation and mediator of the DNA damage response, are being evaluated in clinical trials for the treatment of cancers. Apigenin was capable of inhibiting the activation of CK2 following γ irradiation in LN18 and U87 malignant glioma cells. Apigenin and siRNA-mediated CK2 protein depletion further inhibited NF-κB activation and altered the Tyr68 phosphorylation of Chk2 kinase, a DNA damage response checkpoint kinase, following irradiation. However, CK2 inhibition did not decrease the ability of these glioma cells to repair double-strand DNA breaks, as assessed by COMET assays and γ-H2Ax staining. Likewise, apigenin and siRNA-induced depletion of CK2 failed to sensitize glioma cells to the cytotoxic effect of 2 to 10 G-rays of γ irradiation, as assessed by clonogenic assays. These results contrast with those found in other cancer types, and urge to prudence regarding the inclusion of malignant glioma patients in clinical trials that assess the radiosensitizing role of CK2 inhibitors in solid cancers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analysis of Variance
  • Apigenin / pharmacology*
  • Casein Kinase II / antagonists & inhibitors*
  • Casein Kinase II / genetics
  • Casein Kinase II / metabolism
  • Cell Line, Tumor / drug effects
  • Cell Line, Tumor / radiation effects
  • Cell Survival / radiation effects
  • Checkpoint Kinase 2
  • DNA Damage*
  • DNA Repair / drug effects
  • Enzyme Activation / radiation effects
  • Gene Knockdown Techniques
  • Glioma / radiotherapy*
  • Humans
  • NF-kappa B / metabolism
  • Protein Serine-Threonine Kinases / metabolism
  • RNA Interference
  • Radiation Tolerance / drug effects
  • Radiation-Sensitizing Agents / pharmacology*
  • Statistics, Nonparametric

Substances

  • NF-kappa B
  • Radiation-Sensitizing Agents
  • Apigenin
  • Checkpoint Kinase 2
  • CHEK2 protein, human
  • Casein Kinase II
  • Protein Serine-Threonine Kinases