Ligand binding induces a conformational change in epidermal growth factor receptor dimers

Growth Factors. 2012 Dec;30(6):394-409. doi: 10.3109/08977194.2012.739619. Epub 2012 Nov 20.

Abstract

The activation of the epidermal growth factor receptor (EGFR) kinase requires ligand binding to the extracellular domain (ECD). Previous reports demonstrate that the EGFR-ECD can be crystallized in two conformations - a tethered monomer or, in the presence of ligand, an untethered back-to-back dimer. We use Biosensor analysis to demonstrate that even in the monomeric state different C-terminal extensions of both truncated (EGFR(1-501))-ECD and full-length EGFR(1-621)-ECD can change the conformation of the ligand-binding site. The binding of a monoclonal antibody mAb806, which recognizes the dimer interface, to the truncated EGFR(1-501)-Fc fusion protein is reduced in the presence of ligand, consistent with a change in conformation. On the cell surface, the presence of erythroblastosis B2 (erbB2) increases the binding of mAb806 to the EGFR. The conformation of the erbB2: EGFR heterodimer interface changes when the cells are treated with epidermal growth factor (EGF). We propose that ligand induces kinase-inactive, pre-formed EGFR dimers and heterodimers to change conformation leading to kinase-active tetramers, where kinase activation occurs via an asymmetric interaction between EGFR dimers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry
  • Biosensing Techniques
  • Cell Line
  • Dimerization
  • Epitopes / chemistry
  • ErbB Receptors / chemistry*
  • Fluorescent Dyes / chemistry
  • HEK293 Cells
  • Humans
  • Kinetics
  • Ligands*
  • Mice
  • Models, Molecular
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Tertiary

Substances

  • Antibodies, Monoclonal
  • Epitopes
  • Fluorescent Dyes
  • Ligands
  • ErbB Receptors