Insights into ErbB signaling from the structure of the ErbB2-pertuzumab complex

Cancer Cell. 2004 Apr;5(4):317-28. doi: 10.1016/s1535-6108(04)00083-2.

Abstract

We have determined the 3.2 A X-ray crystal structure of the extracellular domain of the human epidermal growth factor receptor 2 (ErbB2 or HER2) in a complex with the antigen binding fragment of pertuzumab, an anti-ErbB2 monoclonal antibody also known as 2C4 or Omnitarg. Pertuzumab binds to ErbB2 near the center of domain II, sterically blocking a binding pocket necessary for receptor dimerization and signaling. The ErbB2-pertuzumab structure, combined with earlier mutagenesis data, defines the pertuzumab residues essential for ErbB2 interaction. To analyze the ErbB2 side of the interface, we have mutated a number of residues contacting pertuzumab and examined the effects of these mutations on pertuzumab binding and ErbB2-ErbB3 heterodimerization. We have also shown that conserved residues previously shown to be necessary for EGF receptor homodimerization may be dispensible for ErbB2-ErbB3 heterodimerization.

Publication types

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

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry*
  • Antibodies, Monoclonal / genetics
  • Antibodies, Monoclonal / metabolism
  • Antibodies, Monoclonal, Humanized
  • Binding Sites
  • Binding Sites, Antibody
  • CHO Cells
  • Cricetinae
  • Crystallography, X-Ray
  • Dimerization
  • Humans
  • Ligands
  • Models, Molecular
  • Mutagenesis, Site-Directed
  • Protein Structure, Tertiary
  • Receptor, ErbB-2 / chemistry*
  • Receptor, ErbB-2 / genetics
  • Receptor, ErbB-2 / metabolism
  • Signal Transduction*

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Ligands
  • Receptor, ErbB-2
  • pertuzumab

Associated data

  • PDB/1S78