EGFR inhibition triggers an adaptive response by co-opting antiviral signaling pathways in lung cancer

Nat Cancer. 2020 Apr;1(4):394-409. doi: 10.1038/s43018-020-0048-0. Epub 2020 Apr 6.

Abstract

EGFR inhibition is an effective treatment in the minority of non-small cell lung cancer (NSCLC) cases harboring EGFR-activating mutations, but not in EGFR wild type (EGFRwt) tumors. Here, we demonstrate that EGFR inhibition triggers an antiviral defense pathway in NSCLC. Inhibiting mutant EGFR triggers Type I IFN-I upregulation via a RIG-I-TBK1-IRF3 pathway. The ubiquitin ligase TRIM32 associates with TBK1 upon EGFR inhibition, and is required for K63-linked ubiquitination and TBK1 activation. Inhibiting EGFRwt upregulates interferons via an NF-κB-dependent pathway. Inhibition of IFN signaling enhances EGFR-TKI sensitivity in EGFR mutant NSCLC and renders EGFRwt/KRAS mutant NSCLC sensitive to EGFR inhibition in xenograft and immunocompetent mouse models. Furthermore, NSCLC tumors with decreased IFN-I expression are more responsive to EGFR TKI treatment. We propose that IFN-I signaling is a major determinant of EGFR-TKI sensitivity in NSCLC and that a combination of EGFR TKI plus IFN-neutralizing antibody could be useful in most NSCLC patients.

Publication types

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

MeSH terms

  • Animals
  • Carcinoma, Non-Small-Cell Lung* / drug therapy
  • Cell Proliferation
  • ErbB Receptors* / antagonists & inhibitors
  • ErbB Receptors* / genetics
  • Humans
  • Lung Neoplasms* / drug therapy
  • Mice
  • Protein Kinase Inhibitors / pharmacology
  • Signal Transduction*

Substances

  • Protein Kinase Inhibitors
  • EGFR protein, human
  • ErbB Receptors