Inhibition of NF-κB improves sensitivity to irradiation and EGFR-TKIs and decreases irradiation-induced lung toxicity

Int J Cancer. 2019 Jan 1;144(1):200-209. doi: 10.1002/ijc.31907. Epub 2018 Oct 31.

Abstract

Resistance to radiotherapy and to EGFR tyrosine kinase inhibitors (EGFR-TKIs), as well as therapy-related lung toxicity, are serious problems in the treatment of lung cancer. NF-κB has been reported to be associated with radioresistance. Therefore, we evaluated its effects on sensitivity to irradiation and to EGFR-TKIs; irradiation-induced lung toxicity; and the effects of irradiation on sensitivity to EGFR-TKIs. We used IKKβ inhibitor IMD 0354 or p65 depletion to explore their effects on sensitivity to irradiation and to EGFR-TKIs in vitro and in vivo. We evaluated the efficacy of IMD 0354 in a radiation-induced pulmonary-fibrosis mouse model. Irradiation enhanced activation and expression of MET and therefore suppressed the sensitivity of lung cancer cells to irradiation or EGFR-TKIs. Inhibition of NF-κB by IMD 0354 or by p65 depletion reversed irradiation-induced MET activation and increased the sensitivity of lung cancer cells to irradiation, to EGFR-TKIs and to the combination thereof in vitro and in vivo. In addition, IMD 0354 significantly reduced lung toxicity in a murine model of irradiation-induced pneumonia and lung fibrosis. These findings indicated that NF-κB inhibition can improve sensitivity to irradiation and to EGFR-TKIs and can decrease irradiation-induced lung toxicity in lung cancer.

Keywords: EGFR-TKIs; NF-κB; irradiation; lung toxicity; resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Animals
  • Benzamides / pharmacology*
  • Cell Line
  • Cell Line, Tumor
  • Chemoradiotherapy / methods
  • ErbB Receptors / antagonists & inhibitors
  • ErbB Receptors / metabolism
  • Humans
  • Lung / drug effects
  • Lung / pathology
  • Lung / radiation effects
  • Lung Neoplasms / therapy*
  • Male
  • Mice, Inbred BALB C
  • Mice, Nude
  • NF-kappa B / antagonists & inhibitors*
  • NF-kappa B / metabolism
  • Protein Kinase Inhibitors / pharmacology*
  • Radiation Tolerance / drug effects
  • Tumor Burden / drug effects
  • Tumor Burden / radiation effects
  • Xenograft Model Antitumor Assays*

Substances

  • Benzamides
  • NF-kappa B
  • Protein Kinase Inhibitors
  • N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide
  • EGFR protein, human
  • ErbB Receptors