c-Jun/AP-1 overexpression reprograms ERα signaling related to tamoxifen response in ERα-positive breast cancer

Oncogene. 2018 May;37(19):2586-2600. doi: 10.1038/s41388-018-0165-8. Epub 2018 Feb 22.

Abstract

A critical mechanism that has been proposed for transcription regulation by estrogen receptor α (ER) is the tethering of ER to DNA via other transcription factors, such as AP-1. However, genome-wide assessment of the overlap in chromatin binding repertoires of these two transcription factors has not been reported. Here, we show that the AP-1 transcription factor c-Jun interacts with ER and that c-Jun chromatin binding shows extensive overlap with ER binding at the global level. Further, we show that c-Jun overexpression reprograms ER chromatin binding and modulates ER-mediated gene regulation. Our data are consistent with a mechanism where estrogen/ER-dependent crosstalk with AP-1 at the transcriptional level is mediated through the tethering of ER to DNA bound AP-1. Additionally, in our system c-Jun overexpression causes reduced sensitivity to tamoxifen in ER+ breast cancer cells. Integrated cistrome, transcriptome, and clinical data reveal TGFBI as a candidate gene which may confer tamoxifen resistance by ER and AP-1 crosstalk. Further, we show that TGFBI expression is elevated in breast cancer compared to normal breast. Together, our data provide a novel genome-wide footprint of ER and AP-1 crosstalk and suggest AP-1 and TGFBI signaling as potential therapeutic targets in AP-1-overexpressing ER-positive breast tumors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Hormonal / pharmacology*
  • Binding Sites
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / genetics
  • Breast Neoplasms / metabolism*
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm
  • Estrogen Receptor alpha / chemistry
  • Estrogen Receptor alpha / metabolism*
  • Extracellular Matrix Proteins / genetics
  • Female
  • Gene Expression Regulation, Neoplastic
  • Gene Regulatory Networks / drug effects
  • Humans
  • MCF-7 Cells
  • Proto-Oncogene Proteins c-fos / chemistry
  • Proto-Oncogene Proteins c-fos / metabolism*
  • Signal Transduction / drug effects
  • Tamoxifen / pharmacology*
  • Transforming Growth Factor beta / genetics
  • Up-Regulation

Substances

  • Antineoplastic Agents, Hormonal
  • ESR1 protein, human
  • Estrogen Receptor alpha
  • Extracellular Matrix Proteins
  • Proto-Oncogene Proteins c-fos
  • Transforming Growth Factor beta
  • Tamoxifen
  • betaIG-H3 protein