Inhibition of the androgen receptor induces a novel tumor promoter, ZBTB46, for prostate cancer metastasis

Oncogene. 2017 Nov 9;36(45):6213-6224. doi: 10.1038/onc.2017.226. Epub 2017 Jul 10.

Abstract

Current therapeutic regimens for prostate cancer focus on targeting androgen receptor (AR) signaling. However, the AR is a key factor in luminal epithelium differentiation and was shown to have a role as a tumor suppressor. Thus, its inhibition may activate oncogenic pathways that contribute to metastatic castration-resistant prostate cancer (CRPC). Herein, we report a novel tumor promoter, ZBTB46, which is negatively regulated by AR signaling via microRNA (miR)-1-mediated downregulation. ZBTB46 is associated with malignant prostate cancer and is essential for metastasis. Its overexpression can overcome the antitumor effects of miR-1 and promote androgen-independent proliferation. We demonstrated that ZBTB46 can transcriptionally regulate SNAI1, a key epithelial-to-mesenchymal transition (EMT) driver, which could contribute to induction of the EMT after androgen-deprivation therapy and metastasis. Our findings are supportive of the model that disruption of AR's function may predispose prostate cancer to progress to metastatic CRPC.

MeSH terms

  • Androgen Receptor Antagonists / pharmacology
  • Animals
  • Benzamides
  • Cell Line, Tumor
  • Cell Proliferation
  • Dihydrotestosterone / pharmacology
  • Down-Regulation / drug effects
  • Heterografts
  • Humans
  • Male
  • Mice
  • Mice, Nude
  • MicroRNAs / genetics
  • MicroRNAs / metabolism
  • Neoplasm Metastasis
  • Nitriles
  • Phenylthiohydantoin / analogs & derivatives
  • Phenylthiohydantoin / pharmacology
  • Prostatic Neoplasms, Castration-Resistant / metabolism*
  • Prostatic Neoplasms, Castration-Resistant / pathology
  • Receptors, Androgen / metabolism*
  • Signal Transduction
  • Snail Family Transcription Factors / biosynthesis
  • Snail Family Transcription Factors / genetics
  • Transcription Factors / biosynthesis*
  • Transcription Factors / genetics
  • Transfection

Substances

  • AR protein, human
  • Androgen Receptor Antagonists
  • Benzamides
  • MIRN1 microRNA, human
  • MicroRNAs
  • Nitriles
  • Receptors, Androgen
  • SNAI1 protein, human
  • Snail Family Transcription Factors
  • Transcription Factors
  • Zbtb46 protein, human
  • Dihydrotestosterone
  • Phenylthiohydantoin
  • enzalutamide