The PARP inhibitor olaparib potentiates the effect of the DNA damaging agent doxorubicin in osteosarcoma

J Exp Clin Cancer Res. 2018 May 21;37(1):107. doi: 10.1186/s13046-018-0772-9.

Abstract

Background: PARP1 facilitates the recovery of DNA-damaged cells by recruiting DNA damage response molecules such as γH2AX and BRCA1/2, and plays a role in resistance to antitumor therapies. Therefore, PARP inhibition being evaluated as an anti-cancer therapy. However, there are limited studies regrading PARP inhibition in osteosarcoma.

Methods: We evaluated the expression of DNA damage response molecules in 35 human osteosarcomas and investigated the effects of co-treatment of the PARP inhibitor, olaparib, and doxorubicin in osteosarcoma cells.

Results: The expression patterns of PARP1, γH2AX, BRCA1, and BRCA2 were significantly associated with shorter survival of osteosarcoma patients. In osteosarcoma cells, knock-down of PARP1 and treatment of olaparib significantly inhibited proliferation of cells and induced apoptosis. Moreover, the anti-tumor effect was more significant with co-treatment of olaparib and doxorubicin in vitro and in vivo.

Conclusions: This study suggests that combined use of a PARP inhibitor with doxorubicin, a DNA damaging agent, might be effective in the treatment of osteosarcoma patients, especially in the poor-prognostic subgroups of osteosarcoma expressing PARP1, γH2AX, or BRCA1/2.

Keywords: Doxorubicin; Olaparib; Osteosarcoma; PARP1; Prognosis.

MeSH terms

  • Adult
  • Animals
  • Antibiotics, Antineoplastic / pharmacology*
  • Apoptosis / genetics
  • Biomarkers
  • Cell Line, Tumor
  • DNA Damage / drug effects*
  • Disease Models, Animal
  • Doxorubicin / pharmacology*
  • Drug Synergism
  • Female
  • Gene Knockout Techniques
  • Humans
  • Immunohistochemistry
  • Kaplan-Meier Estimate
  • Male
  • Mice
  • Middle Aged
  • Osteosarcoma / drug therapy
  • Osteosarcoma / genetics
  • Osteosarcoma / metabolism
  • Osteosarcoma / pathology
  • Phthalazines / pharmacology*
  • Piperazines / pharmacology*
  • Poly(ADP-ribose) Polymerase Inhibitors / pharmacology*
  • Prognosis
  • Proportional Hazards Models
  • ROC Curve
  • Tissue Array Analysis
  • Xenograft Model Antitumor Assays
  • Young Adult

Substances

  • Antibiotics, Antineoplastic
  • Biomarkers
  • Phthalazines
  • Piperazines
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Doxorubicin
  • olaparib