Inhibitors of histone deacetylases induce tumor-selective cytotoxicity through modulating Aurora-A kinase

J Mol Med (Berl). 2008 Jan;86(1):117-28. doi: 10.1007/s00109-007-0260-8. Epub 2007 Sep 13.

Abstract

The molecular basis of the antitumor selectivity of histone deacetylase inhibitors (HDIs) remains unclear. Centrosomal Aurora-A kinase regulates chromosomal segregation during mitosis. The overexpression or amplification of Aurora-A leads to genetic instability, and its inhibition has shown significant antitumor effects. In this paper, we report that structurally related hydroxamate LAQ824 and SK-7068 induce tumor-selective mitotic defects by depleting Aurora-A. We found that HDI-treated cancer cells, unlike nontransformed cells, exhibit defective mitotic spindles. After HDI, Aurora-A was selectively downregulated in cancer cells, whereas Aurora-B remained unchanged in both cancer and nontransformed cells. LAQ824 or SK-7068 treatment inhibited histone deacetylase (HDAC) 6 present in Aurora-A/heat shock protein (Hsp) 90 complex. Inhibition of HDAC6 acetylated Hsp90 and resulted in dissociation of acetylated Hsp90 from Aurora-A. As a result, Hsp70 binding to Aurora-A was enhanced in cancer cells, leading to proteasomal degradation of Aurora-A. Overall, these provide a novel molecular basis of tumor selectivity of HDI. LAQ824 and SK-7068 might be more effective HDIs in cancer cells with Aurora-A overexpression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents
  • Aurora Kinase B
  • Aurora Kinases
  • Biphenyl Compounds / pharmacology
  • Cell Death / drug effects
  • Cell Line, Tumor
  • Enzyme Inhibitors / pharmacology*
  • HSP70 Heat-Shock Proteins / metabolism
  • HSP90 Heat-Shock Proteins / metabolism
  • Histone Deacetylase 6
  • Histone Deacetylase Inhibitors*
  • Histone Deacetylases
  • Humans
  • Hydroxamic Acids / pharmacology
  • Protein Serine-Threonine Kinases / drug effects
  • Protein Serine-Threonine Kinases / metabolism*
  • Pyrrolidines / pharmacology
  • Stomach Neoplasms / drug therapy
  • Stomach Neoplasms / pathology

Substances

  • Antineoplastic Agents
  • Biphenyl Compounds
  • Enzyme Inhibitors
  • HSP70 Heat-Shock Proteins
  • HSP90 Heat-Shock Proteins
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • LAQ824
  • Pyrrolidines
  • SK-7068
  • AURKB protein, human
  • Aurora Kinase B
  • Aurora Kinases
  • Protein Serine-Threonine Kinases
  • HDAC6 protein, human
  • Histone Deacetylase 6
  • Histone Deacetylases