Growth factor stimulation induces a distinct ER(alpha) cistrome underlying breast cancer endocrine resistance

Genes Dev. 2010 Oct 1;24(19):2219-27. doi: 10.1101/gad.1944810.

Abstract

Estrogen receptor α (ERα) expression in breast cancer is predictive of response to endocrine therapy; however, resistance is common in ERα-positive tumors that overexpress the growth factor receptor ERBB2. Even in the absence of estrogen, ERα can be activated by growth factors, including the epidermal growth factor (EGF). EGF induces a transcriptional program distinct from estrogen; however, the mechanism of the stimulus-specific response is unknown. Here we show that the EGF-induced ERα genomic targets, its cistromes, are distinct from those induced by estrogen in a process dependent on the transcription factor AP-1. The EGF-induced ERα cistrome specifically regulates genes found overexpressed in ERBB2-positive human breast cancers. This provides a potential molecular explanation for the endocrine therapy resistance seen in ERα-positive breast cancers that overexpress ERBB2. These results suggest a central role for ERα in hormone-refractory breast tumors dependent on growth factor pathway activation and favors the development of therapeutic strategies completely antagonizing ERα, as opposed to blocking its estrogen responsiveness alone.

Publication types

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

MeSH terms

  • Breast Neoplasms / physiopathology*
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm / genetics*
  • Epidermal Growth Factor / metabolism*
  • Estrogen Receptor alpha / genetics*
  • Estrogen Receptor alpha / metabolism*
  • Female
  • Gene Expression Regulation, Neoplastic*
  • Humans
  • Receptor, ErbB-2 / metabolism

Substances

  • Estrogen Receptor alpha
  • Epidermal Growth Factor
  • ERBB2 protein, human
  • Receptor, ErbB-2