Shedding of soluble epidermal growth factor receptor (sEGFR) is mediated by a metalloprotease/fibronectin/integrin axis and inhibited by cetuximab

Biochemistry. 2013 Jul 2;52(26):4531-40. doi: 10.1021/bi400437d. Epub 2013 Jun 21.

Abstract

Soluble epidermal growth factor receptor (sEGFR) is a circulating serum biomarker in cancer patients. Recent studies suggest that baseline serum sEGFR concentrations may predict responsiveness to EGFR-targeted therapy. Here, we demonstrate that sEGFR is generated through proteolytic cleavage of a cell surface precursor of an alternately spliced EGF receptor isoform and that sEGFR binds to EGF with high affinity. Proteolytic cleavage is stimulated by an anti-α5/β1 integrin antibody and 4-aminophenylmercuric acetate, and inhibited by fibronectin. Two FDA-approved therapeutic anti-EGFR antibodies also inhibit shedding of sEGFR, thus implicating the cell surface precursor of sEGFR as a competing target for anti-EGFR antibodies in human tissues. These observations parallel trastuzumab regulation of HER2 shedding and have implications for patient stratification in future clinical trials of EGFR-targeted antibodies.

Publication types

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

MeSH terms

  • Alternative Splicing / drug effects
  • Animals
  • Antibodies, Anti-Idiotypic / administration & dosage
  • Antibodies, Monoclonal, Humanized / administration & dosage*
  • Biomarkers, Tumor / chemistry
  • CHO Cells
  • Cetuximab
  • Clinical Trials as Topic
  • Cricetinae
  • Epidermal Growth Factor* / chemistry
  • Epidermal Growth Factor* / metabolism
  • ErbB Receptors* / blood
  • ErbB Receptors* / chemistry
  • Humans
  • Integrins / antagonists & inhibitors
  • Integrins / chemistry*
  • Integrins / immunology
  • Neoplasms / blood
  • Neoplasms / drug therapy
  • Neoplastic Cells, Circulating / chemistry*
  • Protein Isoforms / chemistry

Substances

  • Antibodies, Anti-Idiotypic
  • Antibodies, Monoclonal, Humanized
  • Biomarkers, Tumor
  • Integrins
  • Protein Isoforms
  • Epidermal Growth Factor
  • EGFR protein, human
  • ErbB Receptors
  • Cetuximab