Inhibition of FOXC2 restores epithelial phenotype and drug sensitivity in prostate cancer cells with stem-cell properties

Oncogene. 2016 Nov 17;35(46):5963-5976. doi: 10.1038/onc.2015.498. Epub 2016 Jan 25.

Abstract

Advanced prostate adenocarcinomas enriched in stem-cell features, as well as variant androgen receptor (AR)-negative neuroendocrine (NE)/small-cell prostate cancers are difficult to treat, and account for up to 30% of prostate cancer-related deaths every year. While existing therapies for prostate cancer such as androgen deprivation therapy (ADT), destroy the bulk of the AR-positive cells within the tumor, eradicating this population eventually leads to castration-resistance, owing to the continued survival of AR-/lo stem-like cells. In this study, we identified a critical nexus between p38MAPK signaling, and the transcription factor Forkhead Box Protein C2 (FOXC2) known to promote cancer stem-cells and metastasis. We demonstrate that prostate cancer cells that are insensitive to ADT, as well as high-grade/NE prostate tumors, are characterized by elevated FOXC2, and that targeting FOXC2 using a well-tolerated p38 inhibitor restores epithelial attributes and ADT-sensitivity, and reduces the shedding of circulating tumor cells in vivo with significant shrinkage in the tumor mass. This study thus specifies a tangible mechanism to target the AR-/lo population of prostate cancer cells with stem-cell properties.

MeSH terms

  • Androgens / metabolism
  • Animals
  • Benzamides
  • Cell Line, Tumor
  • Disease Models, Animal
  • Drug Resistance, Neoplasm*
  • Epithelial-Mesenchymal Transition / genetics
  • Epithelium / metabolism*
  • Epithelium / pathology*
  • Forkhead Transcription Factors / genetics
  • Forkhead Transcription Factors / metabolism*
  • Gene Expression
  • Humans
  • MAP Kinase Signaling System / drug effects
  • Male
  • Mice
  • Models, Biological
  • Neoplasm Grading
  • Neoplastic Stem Cells / drug effects*
  • Neoplastic Stem Cells / metabolism*
  • Nitriles
  • Phenotype
  • Phenylthiohydantoin / analogs & derivatives
  • Phenylthiohydantoin / pharmacology
  • Prostate-Specific Antigen / metabolism
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / metabolism*
  • Prostatic Neoplasms / pathology*
  • Receptors, Androgen / metabolism
  • Recurrence
  • Xenograft Model Antitumor Assays
  • Zinc Finger E-box-Binding Homeobox 1 / metabolism

Substances

  • Androgens
  • Benzamides
  • Forkhead Transcription Factors
  • Nitriles
  • Receptors, Androgen
  • ZEB1 protein, human
  • Zinc Finger E-box-Binding Homeobox 1
  • mesenchyme fork head 1 protein
  • Phenylthiohydantoin
  • enzalutamide
  • Prostate-Specific Antigen