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Differential binding patterns of monoclonal antibody 2C4 to the ErbB3-p185her2/neu and the EGFR-p185her2/neu

Z Cai1, G Zhang, Z Zhou

  • 1Department of Pathology/Lab Medicine, University of Pennsylvania School of Medicine, Hamilton Walk, Philadelphia, PA 19104, USA.

Oncogene
|February 12, 2008
PubMed

Insights

Pertuzumab (2C4) targets HER2-positive breast cancer by disrupting HER2-ErbB3 interactions. However, it also associates with the EGFR-HER2 complex, suggesting combination therapies may be more effective.

Area of Science:

  • Oncology
  • Molecular Biology
  • Immunology

Background:

  • HER2 (human epidermal growth factor receptor 2) is overexpressed in approximately 30% of invasive breast cancers.
  • Pertuzumab (2C4) is a monoclonal antibody targeting p185(HER2/neu) and is in Phase II clinical trials.
  • Pertuzumab has been reported to inhibit the association between p185(HER2/neu) and ErbB3.

Purpose of the Study:

  • To investigate the interaction of Pertuzumab (2C4) with the epidermal growth factor receptor (EGFR)-p185(HER2/neu) receptor complex.
  • To evaluate the potential of Pertuzumab as a universal heterodimerization blocker for p185(HER2/neu).

Main Methods:

  • Studied the effects of Pertuzumab (2C4) on EGFR-p185(HER2/neu) heterodimerization.
  • Analyzed the association of 2C4 with the EGFR-p185(HER2/neu) receptor complex.

Main Results:

  • Pertuzumab (2C4) was observed to form associations with the EGFR-p185(HER2/neu) receptor complex.
  • The data suggest that 2C4 does not act as a universal blocker of p185(HER2/neu) heterodimerization.

Conclusions:

  • Pertuzumab's interaction profile indicates it may not be a universal heterodimerization inhibitor for p185(HER2/neu).
  • Combination therapies using multiple monoclonal antibodies targeting distinct surfaces of p185(HER2/neu) are proposed as a potent targeted therapy strategy.

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