A dominant-negative N-terminal fragment of HER2 frequently expressed in breast cancers

Oncogene. 2013 Mar 14;32(11):1452-9. doi: 10.1038/onc.2012.152. Epub 2012 May 28.

Abstract

The transmembrane tyrosine kinase HER2 (ErbB2, neu) is a prototypical biomarker for breast cancers and a therapeutic target. Although anti-HER2 therapies are remarkably effective, HER2-positive tumors are heterogeneous and some subtypes do not respond or develop resistance to these therapies. Here we show that H2NTF, a novel N-terminal fragment of HER2, is expressed at variable levels in 60% of the breast cancer samples analyzed. Characterization of H2NTF shows that it is devoid of the tyrosine kinase domain but it readily interacts with full-length HER2 and other HER receptors. As a consequence, H2NTF acts as a dominant-negative, attenuating the signaling triggered by full-length HER receptors. Expression of H2NTF results in resistance to the treatment with low concentrations of trastuzumab in vitro. However, cells expressing H2NTF and non-expressing cells have similar sensitivity to trastuzumab in vivo, indicating that H2NTF/trastuzumab complexes trigger antibody-dependent cell-mediated cytotoxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Breast Neoplasms / epidemiology
  • Breast Neoplasms / genetics*
  • Carcinoma / epidemiology
  • Carcinoma / genetics*
  • Female
  • Gene Expression Regulation, Neoplastic
  • Gene Frequency
  • Genes, Dominant
  • HEK293 Cells
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred NOD
  • Mice, Nude
  • Mice, SCID
  • Models, Biological
  • Molecular Sequence Data
  • Protein Isoforms / chemistry
  • Protein Isoforms / genetics
  • Protein Structure, Tertiary / genetics
  • Protein Structure, Tertiary / physiology
  • Receptor, ErbB-2 / chemistry*
  • Receptor, ErbB-2 / genetics*
  • Receptor, ErbB-2 / metabolism
  • Tumor Cells, Cultured

Substances

  • Protein Isoforms
  • ERBB2 protein, human
  • Receptor, ErbB-2