The impact of arsenic trioxide and all-trans retinoic acid on p53 R273H-codon mutant glioblastoma

Tumour Biol. 2014 May;35(5):4567-80. doi: 10.1007/s13277-013-1601-6. Epub 2014 Jan 8.

Abstract

Glioblastoma (GBM) is the most common primary brain tumor in adults and demonstrates a 1-year median survival time. Codon-specific hotspot mutations of p53 result in constitutively active mutant p53, which promotes aberrant proliferation, anti-apoptosis, and cell cycle checkpoint failure in GBM. Recently identified CD133(+) cancer stem cell populations (CSC) within GBM also confer therapeutic resistance. We studied targeted therapy in a codon-specific p53 mutant (R273H) created by site-directed mutagenesis in U87MG. The effects of arsenic trioxide (ATO, 1 μM) and all-trans retinoic acid (ATRA, 10 μM), possible targeted treatments of CSCs, were investigated in U87MG neurospheres. The results showed that U87-p53(R273H) cells generated more rapid neurosphere growth than U87-p53(wt) but inhibition of neurosphere proliferation was seen with both ATO and ATRA. U87-p53(R273H) neurospheres showed resistance to differentiation into glial cells and neuronal cells with ATO and ATRA exposure. ATO was able to generate apoptosis at high doses and proliferation of U87-p53(wt) and U87-p53(R273H) cells was reduced with ATO and ATRA in a dose-dependent manner. Elevated pERK1/2 and p53 expression was seen in U87-p53(R273H) neurospheres, which could be reduced with ATO and ATRA treatment. Additionally, differential responses in pERK1/2 were seen with ATO treatment in neurospheres and non-neurosphere cells. In conclusion, codon-specific mutant p53 conferred a more aggressive phenotype to our CSC model. However, ATO and ATRA could potently suppress CSC properties in vitro and may support further clinical investigation of these agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Arsenic Trioxide
  • Arsenicals / pharmacology*
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / genetics
  • Cell Differentiation / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Codon*
  • Extracellular Signal-Regulated MAP Kinases / physiology
  • Genes, p53*
  • Glioblastoma / drug therapy*
  • Glioblastoma / genetics
  • Humans
  • Molecular Sequence Data
  • Mutation*
  • Neoplastic Stem Cells / pathology
  • Oxides / pharmacology*
  • Tretinoin / pharmacology*

Substances

  • Antineoplastic Agents
  • Arsenicals
  • Codon
  • Oxides
  • Tretinoin
  • Extracellular Signal-Regulated MAP Kinases
  • Arsenic Trioxide