NRF2 Regulates HER1 Signaling Pathway to Modulate the Sensitivity of Ovarian Cancer Cells to Lapatinib and Erlotinib

Oxid Med Cell Longev. 2017:2017:1864578. doi: 10.1155/2017/1864578. Epub 2017 Dec 19.

Abstract

NF-E2-related factor 2 (NRF2) regulates the transcription of a battery of metabolic and cytoprotective genes. NRF2 and epidermal growth factor receptors (EGFRs/HERs) are regulators of cellular proliferation and determinants of cancer initiation and progression. NRF2 and HERs confer cancers with resistance to several therapeutic agents. Nevertheless, there is limited understanding of the regulation of HER expression and activation and the link between NRF2 and HER signalling pathways. We show that NRF2 regulates both basal and inducible expression of HER1, as treatment of ovarian cancer cells (PEO1, OVCAR3, and SKOV3) with NRF2 activator tBHQ inducing HER1, while inhibition of NRF2 by siRNA knockdown or with retinoid represses HER1. Furthermore, treatment of cells with tBHQ increased total and phosphorylated NRF2, HER1, and AKT levels and compromised the cytotoxic effect of lapatinib or erlotinib. Treatment with siRNA or retinoid antagonised the effect of tBHQ on NRF2 and HER1 levels and enhanced the sensitivity of ovarian cancer cells to lapatinib or erlotinib. Pharmacological or genetic inhibition of NRF2 and/or treatment with lapatinib or erlotinib elevated cellular ROS and depleted glutathione. This extends the understanding of NRF2 and its regulation of HER family receptors and opens a strategic target for improving cancer therapy.

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Bexarotene
  • Cell Line, Tumor
  • Down-Regulation / drug effects
  • ErbB Receptors / biosynthesis
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism*
  • Erlotinib Hydrochloride / administration & dosage
  • Erlotinib Hydrochloride / pharmacology*
  • Female
  • Humans
  • Lapatinib
  • MCF-7 Cells
  • NF-E2-Related Factor 2 / antagonists & inhibitors
  • NF-E2-Related Factor 2 / genetics
  • NF-E2-Related Factor 2 / metabolism*
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / metabolism*
  • Ovarian Neoplasms / pathology
  • Protein Kinase Inhibitors / administration & dosage
  • Protein Kinase Inhibitors / pharmacology
  • Quinazolines / administration & dosage
  • Quinazolines / pharmacology*
  • RNA, Small Interfering / administration & dosage
  • RNA, Small Interfering / genetics
  • Reactive Oxygen Species / metabolism
  • Signal Transduction
  • Tetrahydronaphthalenes / administration & dosage
  • Tetrahydronaphthalenes / pharmacology

Substances

  • NF-E2-Related Factor 2
  • NFE2L2 protein, human
  • Protein Kinase Inhibitors
  • Quinazolines
  • RNA, Small Interfering
  • Reactive Oxygen Species
  • Tetrahydronaphthalenes
  • Lapatinib
  • Bexarotene
  • Erlotinib Hydrochloride
  • EGFR protein, human
  • ErbB Receptors