Bivalence of EGF-like ligands drives the ErbB signaling network

EMBO J. 1997 Aug 15;16(16):4938-50. doi: 10.1093/emboj/16.16.4938.

Abstract

Signaling by epidermal growth factor (EGF)-like ligands is mediated by an interactive network of four ErbB receptor tyrosine kinases, whose mechanism of ligand-induced dimerization is unknown. We contrasted two existing models: a conformation-driven activation of a receptor-intrinsic dimerization site and a ligand bivalence model. Analysis of a Neu differentiation factor (NDF)-induced heterodimer between ErbB-3 and ErbB-2 favors a bivalence model; the ligand simultaneously binds both ErbB-3 and ErbB-2, but, due to low-affinity of the second binding event, ligand bivalence drives dimerization only when the receptors are membrane anchored. Results obtained with a chimera and isoforms of NDF/neuregulin predict that each terminus of the ligand molecule contains a distinct binding site. The C-terminal low-affinity site has broad specificity, but it prefers interaction with ErbB-2, an oncogenic protein acting as a promiscuous low-affinity subunit of the three primary receptors. Thus, ligand bivalence enables signal diversification through selective recruitment of homo- and heterodimers of ErbB receptors, and it may explain oncogenicity of erbB-2/HER2.

Publication types

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

MeSH terms

  • Animals
  • Binding Sites
  • CHO Cells
  • Cricetinae
  • Dimerization
  • Epidermal Growth Factor / chemistry
  • Epidermal Growth Factor / genetics
  • Epidermal Growth Factor / metabolism*
  • ErbB Receptors / chemistry
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism*
  • Glycoproteins / chemistry
  • Glycoproteins / metabolism*
  • Humans
  • Kinetics
  • Ligands
  • Models, Molecular
  • Mutagenesis
  • Neuregulins
  • Protein-Tyrosine Kinases / metabolism
  • Proto-Oncogene Proteins / chemistry
  • Proto-Oncogene Proteins / metabolism*
  • Receptor, ErbB-2 / chemistry
  • Receptor, ErbB-2 / metabolism*
  • Receptor, ErbB-3
  • Recombinant Proteins / metabolism
  • Signal Transduction*

Substances

  • Glycoproteins
  • Ligands
  • Neuregulins
  • Proto-Oncogene Proteins
  • Recombinant Proteins
  • biregulin
  • Epidermal Growth Factor
  • ErbB Receptors
  • Protein-Tyrosine Kinases
  • Receptor, ErbB-2
  • Receptor, ErbB-3

Associated data

  • PDB/1HRE