Silencing of androgen-regulated genes using a fusion of AR with the PLZF transcriptional repressor

Oncogene. 2004 Sep 30;23(45):7561-70. doi: 10.1038/sj.onc.1208030.

Abstract

The androgen receptor (AR) is a member of the nuclear receptor superfamily of ligand-activated transcription factors and plays a key role in the development and progression of prostate cancer. Current therapies include the use of antiandrogens aimed at inhibiting the transcriptional activation of AR-regulated genes by AR. Here, we explore a strategy aimed at obtaining silencing of AR-regulated genes, based on the properties of the transcriptional repressor promyelocytic leukamia zinc-finger protein (PLZF). In order to do this, we have made a fusion protein between PLZF and AR, named PLZF-AR, and show that PLZF-AR is able to bring about silencing of genomically encoded AR-regulated genes and inhibit the androgen-regulated growth of LNCaP prostate cancer cells. Together, our results show that this strategy is able to bring about potent repression of AR-regulated responses and, therefore, could be of value in the development of new therapies for prostate cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androgens / physiology*
  • Animals
  • Base Sequence
  • COS Cells
  • DNA Primers
  • DNA-Binding Proteins / genetics*
  • Fluorescent Antibody Technique, Indirect
  • Gene Expression Regulation / physiology*
  • Gene Silencing*
  • Genes, Reporter
  • Humans
  • Kruppel-Like Transcription Factors
  • Promyelocytic Leukemia Zinc Finger Protein
  • Receptors, Androgen / genetics*
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / physiology*
  • Transcription Factors / genetics*

Substances

  • Androgens
  • DNA Primers
  • DNA-Binding Proteins
  • Kruppel-Like Transcription Factors
  • Promyelocytic Leukemia Zinc Finger Protein
  • Receptors, Androgen
  • Recombinant Fusion Proteins
  • Transcription Factors
  • ZBTB16 protein, human