Poly(ADPR)polymerase-1 signalling of the DNA damage induced by DNA topoisomerase I poison in D54(p53wt) and U251(p53mut) glioblastoma cell lines

Pharmacol Res. 2007 Jan;55(1):49-56. doi: 10.1016/j.phrs.2006.10.005. Epub 2006 Oct 20.

Abstract

Glioblastomas are widely characterised by the mutation of the p53 gene and p53 disruption sensitizes glioblastoma cells to DNA topoisomerase I (TOPO I) inhibitor-mediated apoptosis. We investigated the effects of combined treatments with the DNA topoisomerase I inhibitor Topotecan and the poly(ADPR)polymerase-1 inhibitor NU1025 in D54(p53wt) and U251(p53mut) glioblastoma cell lines. Analysis of cell growth and cell cycle kinetics showed a synergistic anti-proliferative effect of 10 nM TPT and 10 microM NU1025 and a G2/M block of the cell cycle. We also evaluated, the influence of TPT+/-NU1025 treatment on PARP-1 and p53 activity. We got evidences of a TPT-dependent increase of PARP-1 auto-modification level in both the cells. Moreover, in the D54(p53wt) cells we found that in co-treatments NU1025 incremented the TPT-dependent stimulation of p53 transcriptional activity and increased the p21 nuclear amount. Conversely, in U251(p53mut) cells we found that NU1025 incremented the TPT-dependent apoptosis characterised by PARP-1 proteolysis. Our findings suggest that the modulation of PARP-1 can be considered a strategy in the potentiation of the chemotherapeutic action of TOPO I poisons in glioblastoma cells apart from their p53 status.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Blotting, Western
  • Brain Neoplasms / enzymology
  • Brain Neoplasms / genetics
  • Brain Neoplasms / physiopathology*
  • Cell Line, Tumor
  • Cell Nucleus / chemistry
  • Cell Nucleus / enzymology
  • DNA Damage / physiology*
  • DNA Topoisomerases, Type I*
  • Densitometry
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Enzyme Inhibitors / poisoning
  • Flow Cytometry
  • Glioblastoma / enzymology
  • Glioblastoma / genetics
  • Glioblastoma / physiopathology*
  • Humans
  • In Situ Nick-End Labeling
  • Indicators and Reagents
  • Mutation / physiology
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerases / physiology*
  • Quinazolines / pharmacology
  • Signal Transduction / drug effects
  • Topotecan / poisoning
  • Tumor Suppressor Protein p53 / genetics

Substances

  • Enzyme Inhibitors
  • Indicators and Reagents
  • NU 1025
  • Quinazolines
  • Tumor Suppressor Protein p53
  • Topotecan
  • PARP1 protein, human
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerases
  • DNA Topoisomerases, Type I