Nkx3-1 and LEF-1 function as transcriptional inhibitors of estrogen receptor activity

Cancer Res. 2008 Sep 15;68(18):7380-5. doi: 10.1158/0008-5472.CAN-08-0133.

Abstract

Estrogen receptor (ER)-associated cofactors and cooperating transcription factors are one of the primary components determining transcriptional activity of estrogen target genes and may constitute potential therapeutic targets. Recent mapping of ER-binding sites on a genome-wide scale has provided insight into novel cooperating factors based on the enrichment of transcription factor motifs within the ER-binding sites. We have used the ER-binding sites in combination with sequence conservation to identify the statistical enrichment of Nkx and LEF motifs. We find that Nkx3-1 and LEF-1 bind to several ER cis-regulatory elements in vivo, but they both function as transcriptional repressors of estrogen signaling. We show that Nkx3-1 and LEF-1 can inhibit ER binding to chromatin, suggesting competition for common chromatin-binding regions. These data provide insight into the role of Nkx3-1 and LEF-1 as potential regulators of the hormone response in breast cancer.

MeSH terms

  • Animals
  • Binding Sites
  • Breast Neoplasms / genetics
  • Cell Line, Tumor
  • Chromatin / genetics
  • Chromatin / metabolism
  • Homeodomain Proteins / biosynthesis
  • Homeodomain Proteins / genetics
  • Homeodomain Proteins / metabolism*
  • Humans
  • Lymphoid Enhancer-Binding Factor 1 / biosynthesis
  • Lymphoid Enhancer-Binding Factor 1 / genetics
  • Lymphoid Enhancer-Binding Factor 1 / metabolism*
  • Mice
  • Plasmids / genetics
  • Protein Binding
  • RNA, Small Interfering / genetics
  • Receptors, Estrogen / antagonists & inhibitors*
  • Receptors, Estrogen / genetics
  • Receptors, Estrogen / metabolism
  • Transcription Factors / biosynthesis
  • Transcription Factors / genetics
  • Transcription Factors / metabolism*
  • Transcription, Genetic
  • Transfection

Substances

  • Chromatin
  • Homeodomain Proteins
  • Lymphoid Enhancer-Binding Factor 1
  • NKX3-1 protein, human
  • Nkx3-1 protein, mouse
  • RNA, Small Interfering
  • Receptors, Estrogen
  • Transcription Factors