The pan-histone deacetylase inhibitor LBH589 (panobinostat) alters the invasive breast cancer cell phenotype

Int J Oncol. 2014 Mar;44(3):700-8. doi: 10.3892/ijo.2013.2218. Epub 2013 Dec 19.

Abstract

Triple-negative breast cancer (TNBC) is a very aggressive type of tumour and its aggressiveness is linked to E-cadherin downregulation. In estrogen-sensitive breast cancer, high levels of E-cadherin fit with high levels of ERα and MTA3 (a component of the transcription Mi-2/NuRD complex with intrinsic DAC activity). In TNBC the E-cadherin downregulation could be due to epigenetic silencing of the CDH1 gene as well as to the lack of a fully functioning ERα-activated pathway. We report that the pan-histone deacetylase inhibitor LBH589, a potent anti-proliferative agent, induced E-cadherin expression on cell membranes of MDA-MB-231 cells (TNBC), determining a reduction of cell invasion and migration. Even though E-cadherin expression in breast cancer is also regulated by estradiol and the ERα/MTA3/Snail/Slug pathway, LBH589 is able to increase E-cadherin without affecting the estrogen pathway. In fact, no expression of ERα, PR and FoxA1 was observed in MDA-MB-231 cells before and after LBH589 treatment; furthermore, the drug caused an increase in Snail and Slug expression with a concomitant reduction of MTA3 levels. Taking into consideration its anti-proliferative and anti-invasive properties, we suggest the use of LBH589 in aggressive breast cancer refractory to hormonal therapy.

MeSH terms

  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / pathology
  • Cadherins / biosynthesis
  • Cell Line, Tumor
  • Epigenesis, Genetic*
  • Estradiol
  • Estrogen Receptor alpha / biosynthesis
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Histone Deacetylase Inhibitors / administration & dosage
  • Humans
  • Hydroxamic Acids / administration & dosage*
  • Indoles / administration & dosage*
  • Neoplasm Invasiveness / genetics*
  • Panobinostat

Substances

  • Cadherins
  • ESR1 protein, human
  • Estrogen Receptor alpha
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Indoles
  • Estradiol
  • Panobinostat