Radiosensitization by the PARP inhibitor olaparib in BRCA1-proficient and deficient high-grade serous ovarian carcinomas

Gynecol Oncol. 2018 Sep;150(3):534-544. doi: 10.1016/j.ygyno.2018.07.002. Epub 2018 Jul 17.

Abstract

Objective: Approximately 15-25% of high-grade serous ovarian carcinomas (HGSOC) harbor BRCA1/2 mutations. Inhibition of Poly (ADP-ribose) polymerase (PARP) is synthetically lethal to cells and tumors with BRCA1/2 mutation. Our goal was to investigate the radiosensitizing effects of PARP inhibitor olaparib in HGSOC with different BRCA1 status.

Methods: The radiosensitizing effects of olaparib were tested on BRCA1-proficient and deficient HGSOC by clonogenic survival and tumor growth assays. The effects of olaparib and radiation on DNA damage, PARP activity, and apoptosis were determined.

Results: BRCA1-deficient HGSOC cells were more sensitive to RT alone and exhibited significantly higher levels of olaparib-mediated radiosensitization compared to BRCA1-proficient cells. Furthermore, when combined with RT, olaparib inhibited DNA damage repair and PARP1 activity, increased apoptosis, decreased growth of HGSOC xenografts and increased overall host survival. The growth-inhibitory effects of the combined olaparib and RT treatment were more pronounced in mice bearing BRCA1-deficient tumors compared to BRCA1-proficient tumors.

Conclusions: These results provide a preclinical rationale for improved treatment modalities using olaparib as an effective radiosensitizer in HGSOC, particularly in tumors with BRCA1-deficiencies.

Keywords: BRCA1; HGSOC; PARP inhibitor; Radiosensitization; Radiotherapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • DNA Damage / drug effects
  • DNA Repair / drug effects
  • Female
  • Genes, BRCA1*
  • Humans
  • Mice
  • Neoplasm Grading
  • Neoplasm Transplantation
  • Neoplasms, Cystic, Mucinous, and Serous / drug therapy*
  • Neoplasms, Cystic, Mucinous, and Serous / genetics
  • Neoplasms, Cystic, Mucinous, and Serous / radiotherapy
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / genetics
  • Ovarian Neoplasms / radiotherapy
  • Phthalazines / pharmacology*
  • Phthalazines / therapeutic use
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use
  • Poly (ADP-Ribose) Polymerase-1 / antagonists & inhibitors
  • Radiation Tolerance / drug effects*

Substances

  • Antineoplastic Agents
  • Phthalazines
  • Piperazines
  • PARP1 protein, human
  • Poly (ADP-Ribose) Polymerase-1
  • olaparib