A tale of the epidermal growth factor receptor: The quest for structural resolution on cells

Methods. 2016 Feb 15:95:86-93. doi: 10.1016/j.ymeth.2015.10.009. Epub 2015 Oct 17.

Abstract

The challenge of determining the architecture and geometry of oligomers of the epidermal growth factor receptor (EGFR) on the cell surface has been approached using a variety of biochemical and biophysical methods. This review is intended to provide a narrative of how key concepts in the field of EGFR research have evolved over the years, from the origins of the prevalent EGFR signalling dimer hypothesis through to the development and implementation of methods that are now challenging the conventional view. The synergy between X-ray crystallography and cellular fluorescence microscopy has become particularly important, precisely because the results from these two methods diverged and highlighted the complexity of the challenge. We illustrate how developments in super-resolution microscopy are now bridging this gap. Exciting times lie ahead where knowledge of the nature of the complexes can assist with the development of a new generation of anti-cancer drugs.

Keywords: EGFR; FRET; Membrane protein structure; Receptor tyrosine kinase; Signal transduction; Single molecule fluorescence microscopy; Super-resolution microscopy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Allosteric Regulation
  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Membrane / chemistry
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Cell Membrane / ultrastructure*
  • Crystallography, X-Ray / methods*
  • Drosophila melanogaster / metabolism
  • ErbB Receptors / antagonists & inhibitors
  • ErbB Receptors / chemistry
  • ErbB Receptors / metabolism
  • ErbB Receptors / ultrastructure*
  • Fluorescence Resonance Energy Transfer / methods*
  • Humans
  • Microscopy, Fluorescence / methods*
  • Molecular Dynamics Simulation
  • Phosphorylation
  • Protein Multimerization
  • Signal Transduction

Substances

  • Antineoplastic Agents
  • EGFR protein, human
  • ErbB Receptors