DAX-1, as an androgen-target gene, inhibits aromatase expression: a novel mechanism blocking estrogen-dependent breast cancer cell proliferation

Cell Death Dis. 2013 Jul 11;4(7):e724. doi: 10.1038/cddis.2013.235.

Abstract

Sexual hormones, estrogens and androgens, determine biological response in a tissue- and gender-specific manner and have a pivotal role in endocrine-mediated tumorigenesis. In situ estrogen production by aromatase is a critical determinant for breast cancer growth and progression. On the contrary, clinical and in vitro studies indicate that androgens have a protective role in mammary carcinogenesis. Here, we demonstrated, in hormone-dependent breast cancer cells, the existence of a functional interplay between the androgen receptor (AR), the orphan nuclear receptor DAX-1 and the aromatase enzyme involved in the inhibition of the estrogen-dependent breast cancer cell proliferation exerted by androgen signaling. Indeed, our results revealed, in MCF-7 cells, that ligand-activated AR induces the expression of the orphan nuclear receptor DAX-1 by direct binding to a newly identified androgen-response-element within the DAX-1 proximal promoter. In turn, androgen-induced DAX-1 is recruited, in association with the corepressor N-CoR, within the SF-1/LRH-1 containing region of the aromatase promoter, thereby repressing aromatase expression and activity. In elucidating a novel mechanism by which androgens, through DAX-1, inhibit aromatase expression in breast cancer cell lines, these findings reinforce the theory of androgen- opposing estrogen-action, opening new avenues for therapeutic intervention in estrogen-dependent breast tumors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androgens / pharmacology
  • Apoptosis
  • Aromatase / genetics
  • Aromatase / metabolism*
  • Base Sequence
  • Breast Neoplasms
  • Cell Proliferation*
  • DAX-1 Orphan Nuclear Receptor / genetics*
  • DAX-1 Orphan Nuclear Receptor / metabolism
  • Enzyme Repression
  • Estrogens / physiology*
  • Female
  • Gene Expression
  • Gene Expression Regulation, Neoplastic
  • Humans
  • MCF-7 Cells
  • Nandrolone / analogs & derivatives
  • Nandrolone / pharmacology
  • Neoplasms, Hormone-Dependent
  • Promoter Regions, Genetic
  • Receptors, Androgen / metabolism
  • Response Elements

Substances

  • Androgens
  • DAX-1 Orphan Nuclear Receptor
  • Estrogens
  • NR0B1 protein, human
  • Receptors, Androgen
  • Nandrolone
  • mibolerone
  • Aromatase
  • CYP19A1 protein, human