Magnitude of Ubiquitination Determines the Fate of Epidermal Growth Factor Receptor Upon Ligand Stimulation

J Mol Biol. 2021 Oct 15;433(21):167240. doi: 10.1016/j.jmb.2021.167240. Epub 2021 Sep 8.

Abstract

Receptor tyrosine kinases (RTK) bind growth factors and are critical for cell proliferation and differentiation. Their dysregulation leads to a loss of growth control, often resulting in cancer. Epidermal growth factor receptor (EGFR) is the prototypic RTK and can bind several ligands exhibiting distinct mitogenic potentials. Whereas the phosphorylation on individual EGFR sites and their roles for downstream signaling have been extensively studied, less is known about ligand-specific ubiquitination events on EGFR, which are crucial for signal attenuation and termination. We used a proteomics-based workflow for absolute quantitation combined with mathematical modeling to unveil potentially decisive ubiquitination events on EGFR from the first 30 seconds to 15 minutes of stimulation. Four ligands were used for stimulation: epidermal growth factor (EGF), heparin-binding-EGF like growth factor, transforming growth factor-α and epiregulin. Whereas only little differences in the order of individual ubiquitination sites were observed, the overall amount of modified receptor differed depending on the used ligand, indicating that absolute magnitude of EGFR ubiquitination, and not distinctly regulated ubiquitination sites, is a major determinant for signal attenuation and the subsequent cellular outcomes.

Keywords: AQUA; mass spectrometry; proteomics; signaling; ubiquitin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Cell Line, Tumor
  • Epidermal Growth Factor / chemistry
  • Epidermal Growth Factor / genetics
  • Epidermal Growth Factor / metabolism*
  • Epiregulin / chemistry
  • Epiregulin / genetics
  • Epiregulin / metabolism*
  • Epithelial Cells / cytology
  • Epithelial Cells / metabolism
  • ErbB Receptors / chemistry
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism
  • Gene Expression
  • Heparin-binding EGF-like Growth Factor / chemistry
  • Heparin-binding EGF-like Growth Factor / genetics
  • Heparin-binding EGF-like Growth Factor / metabolism*
  • Humans
  • Ligands
  • Models, Molecular
  • Mutation
  • Phosphorylation
  • Protein Conformation
  • Protein Processing, Post-Translational
  • Proteomics
  • Signal Transduction / genetics*
  • Transforming Growth Factor alpha / chemistry
  • Transforming Growth Factor alpha / genetics
  • Transforming Growth Factor alpha / metabolism*
  • Ubiquitination

Substances

  • EREG protein, human
  • Epiregulin
  • HBEGF protein, human
  • Heparin-binding EGF-like Growth Factor
  • Ligands
  • TGFA protein, human
  • Transforming Growth Factor alpha
  • Epidermal Growth Factor
  • EGFR protein, human
  • ErbB Receptors