Erlotinib protects against LPS-induced endotoxicity because TLR4 needs EGFR to signal

Proc Natl Acad Sci U S A. 2015 Aug 4;112(31):9680-5. doi: 10.1073/pnas.1511794112. Epub 2015 Jul 20.

Abstract

Several components of the canonical pathway of response to lipopolysaccharide (LPS) are required for the EGF-dependent activation of NFκB. Conversely, the ability of Toll-like Receptor 4 (TLR4) to activate NFκB in response to LPS is impaired by down regulating EGF receptor (EGFR) expression or by using the EGFR inhibitor erlotinib. The LYN proto-oncogene (LYN) is required for signaling in both directions. LYN binds to the EGFR upon LPS stimulation, and erlotinib impairs this association. In mice, erlotinib blocks the LPS-induced expression of tumor necrosis factor α (TNFα) and interleukin-6 (IL-6) and ameliorates LPS-induced endotoxity, revealing that EGFR is essential for LPS-induced signaling in vivo.

Keywords: EGFR; LPS; NFκB; TLR4; erlotinib.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cell Line
  • Cytokines / metabolism
  • Epidermal Growth Factor / pharmacology
  • ErbB Receptors / metabolism*
  • Erlotinib Hydrochloride
  • Gene Silencing / drug effects
  • Humans
  • Lipopolysaccharides / toxicity*
  • MAP Kinase Kinase Kinases / metabolism
  • Mice
  • Myeloid Differentiation Factor 88 / metabolism
  • NF-kappa B / metabolism
  • Phosphorylation / drug effects
  • Protective Agents / pharmacology*
  • Proto-Oncogene Mas
  • Quinazolines / pharmacology*
  • Signal Transduction / drug effects*
  • Toll-Like Receptor 4 / metabolism*
  • Tumor Necrosis Factor-alpha / pharmacology
  • src-Family Kinases / metabolism

Substances

  • Cytokines
  • Lipopolysaccharides
  • MAS1 protein, human
  • Myeloid Differentiation Factor 88
  • NF-kappa B
  • Protective Agents
  • Proto-Oncogene Mas
  • Quinazolines
  • TLR4 protein, human
  • Toll-Like Receptor 4
  • Tumor Necrosis Factor-alpha
  • Epidermal Growth Factor
  • Erlotinib Hydrochloride
  • ErbB Receptors
  • lyn protein-tyrosine kinase
  • src-Family Kinases
  • MAP Kinase Kinase Kinases
  • MAP kinase kinase kinase 7