Specific activation of the p53 pathway by low dose actinomycin D: a new route to p53 based cyclotherapy

Cell Cycle. 2009 Sep 1;8(17):2810-8. doi: 10.4161/cc.8.17.9503. Epub 2009 Sep 13.

Abstract

The activation of p53 has been proposed as a novel anti-cancer treatment in two distinct contexts. In the first activation of p53 in tumor cells can promote apoptosis and senescence and enhance the anti-tumor activity of cytotoxic chemotherapeutic drugs. In the second application activation of p53 in normal tissues can cause a reversible cell cycle arrest that can be used to protect normal cells from the action of anti-mitotics. In this cyclotherapy role p53 mutant tumor cells are not arrested and remain sensitive to anti-mitotics. The advent of specific p53 activating molecules such as nutlin-3 has encouraged both approaches. We have sought for a clinically approved drug that can mimic nutlin-3. We show here that low doses of actinomycin D mimic nutlin-3 in the highly specific activation of p53 dependant transcription, in the induction of a reversible protective growth arrest in normal cells and in the enhancement of the activity of chemotherapeutic drug induced killing of p53 positive human tumor cells. While high doses of actinomycin D reveal its more non-specific activities, low doses of the drug will allow exploration of the value of p53 activation in preclinical and clinical models before nutlin-3 like drugs are approved.

MeSH terms

  • Antibiotics, Antineoplastic / pharmacology*
  • Apoptosis
  • Cell Cycle
  • Cell Line, Tumor
  • Dactinomycin / pharmacology*
  • Gene Expression Profiling
  • Humans
  • Imidazoles / pharmacology
  • Phosphorylation
  • Piperazines / pharmacology
  • Time Factors
  • Tumor Suppressor Protein p53 / genetics
  • Tumor Suppressor Protein p53 / metabolism*

Substances

  • Antibiotics, Antineoplastic
  • Imidazoles
  • Piperazines
  • Tumor Suppressor Protein p53
  • Dactinomycin
  • nutlin 3