The HOXB7 protein renders breast cancer cells resistant to tamoxifen through activation of the EGFR pathway

Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2736-41. doi: 10.1073/pnas.1018859108. Epub 2011 Jun 20.

Abstract

Multiple factors including long-term treatment with tamoxifen are involved in the development of selective estrogen receptor (ER) modulator resistance in ERα-positive breast cancer. Many underlying molecular events that confer resistance are known but a unifying theme is yet to be revealed. In this report, we provide evidence that HOXB7 overexpression renders MCF-7 cells resistant to tamoxifen via cross-talk between receptor tyrosine kinases and ERα signaling. HOXB7 is an ERα-responsive gene. Extended treatment of MCF-7 cells with tamoxifen resulted in progressively increasing levels of HOXB7 expression, along with EGFR and EGFR ligands. Up-regulation of EGFR occurs through direct binding of HOXB7 to the EGFR promoter, enhancing transcriptional activity. Finally, higher expression levels of HOXB7 in the tumor significantly correlated with poorer disease-free survival in ERα-positive patients with breast cancer on adjuvant tamoxifen monotherapy. These studies suggest that HOXB7 acts as a key regulator, orchestrating a major group of target molecules in the oncogenic hierarchy. Functional antagonism of HOXB7 could circumvent tamoxifen resistance.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / metabolism*
  • Cell Line, Tumor
  • Cell Transformation, Neoplastic / genetics
  • Cell Transformation, Neoplastic / pathology
  • Drug Resistance, Neoplasm / drug effects*
  • Enzyme Activation / drug effects
  • ErbB Receptors / metabolism*
  • Estrogen Receptor alpha / metabolism
  • Estrogens / pharmacology
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Homeodomain Proteins / genetics
  • Homeodomain Proteins / metabolism*
  • Humans
  • Kaplan-Meier Estimate
  • Mice
  • Prognosis
  • Signal Transduction / drug effects
  • Tamoxifen / pharmacology*
  • Tamoxifen / therapeutic use*

Substances

  • ESR1 protein, human
  • Estrogen Receptor alpha
  • Estrogens
  • HOXB7 protein, human
  • Homeodomain Proteins
  • Tamoxifen
  • EGFR protein, human
  • ErbB Receptors