Inhibiting estrogen responses in breast cancer cells using a fusion protein encoding estrogen receptor-alpha and the transcriptional repressor PLZF

Gene Ther. 2005 Mar;12(5):452-60. doi: 10.1038/sj.gt.3302421.

Abstract

Estrogen receptor alpha (ERalpha) is a ligand-inducible transcription factor that acts to regulate gene expression by binding to palindromic DNA sequence, known as the estrogen response element, in promoters of estrogen-regulated genes. In breast cancer ERalpha plays a central role, where estrogen-regulated gene expression leads to tumor initiation, growth and survival. As an approach to silencing estrogen-regulated genes, we have studied the activities of a fusion protein between ERalpha and the promyelocytic leukemia zinc-finger (PLZF) protein, a transcriptional repressor that acts through chromatin remodeling. To do this, we have developed lines from the estrogen-responsive MCF-7 breast cancer cell line in which the expression of the fusion protein PLZF-ERalpha is conditionally regulated by tetracycline and shows that these feature long-term silencing of the expression of several well-characterized estrogen-regulated genes, namely pS2, cathepsin-D and the progesterone receptor. However, the estrogen-regulated growth of these cells is not inhibited unless PLZF-ERalpha expression is induced, an observation that we have confirmed both in vitro and in vivo. Taken together, these results show that PLZF-ERalpha is a potent repressor of estrogen-regulated gene expression and could be useful in distinguishing estrogen-regulated genes required for the growth of breast cancer cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Breast Neoplasms / metabolism*
  • Breast Neoplasms / therapy*
  • Cell Line, Tumor
  • DNA-Binding Proteins / genetics*
  • DNA-Binding Proteins / metabolism
  • Estrogen Receptor alpha / genetics*
  • Estrogen Receptor alpha / metabolism
  • Estrogens / metabolism*
  • Female
  • Gene Expression Regulation
  • Genetic Therapy / methods*
  • Humans
  • Kruppel-Like Transcription Factors
  • Luciferases / genetics
  • Mice
  • Mice, Nude
  • Promyelocytic Leukemia Zinc Finger Protein
  • Recombinant Fusion Proteins / therapeutic use*
  • Transcription Factors / genetics*
  • Transcription Factors / metabolism
  • Transfection / methods
  • beta-Galactosidase / genetics

Substances

  • DNA-Binding Proteins
  • Estrogen Receptor alpha
  • Estrogens
  • Kruppel-Like Transcription Factors
  • Promyelocytic Leukemia Zinc Finger Protein
  • Recombinant Fusion Proteins
  • Transcription Factors
  • Zbtb16 protein, mouse
  • ZBTB16 protein, human
  • Luciferases
  • beta-Galactosidase