提拉帕扎明
癌症研究
缺氧(环境)
聚ADP核糖聚合酶
肿瘤缺氧
医学
癌症
化学
放射治疗
氧气
体外
内科学
细胞毒性
DNA
生物化学
有机化学
聚合酶
作者
Manal Mehibel,Jimmy Yu Xu,Grace Li,Jung Joo Moon,Kaushik N. Thakkar,Anh N. Diep,Ryan Kim,Joshua Bloomstein,Siren Xiao,Julien Bacal,Joshua C. Saldivar,Quynh‐Thu Le,Karlene A. Cimprich,Erinn B. Rankin,Amato Giaccia
标识
DOI:10.1158/1557-3265.radsci21-ia-003
摘要
Abstract Severe hypoxia causes resistance to conventional chemotherapy and has been reported to synergize with PARP inhibitors (PARPi) through suppression of homologous recombination (HR). While this synergistic killing is true at oxygen levels less than 0.5%, our study shows that less severe hypoxia (e.g. 2% oxygen) is instead associated with resistance to PARPi in HR proficient cells. Interestingly, we demonstrate that HR deficient hypoxic tumors are significantly less responsive to PARPi, due to limited ROS-induced intrinsic DNA damage. To determine the contribution of hypoxic cells to PARPi, we used the hypoxic cytotoxin Tirapazamine to target hypoxic tumor cells. We found that the elimination of hypoxic tumor cells by Tirapazamine led to a substantial antitumor response with PARPi compared to PARPi treated tumors alone, without enhancing normal tissue toxicity. These studies indicate that tumor hypoxia reduces the efficacy of PARPi to tumor cells and that eliminating hypoxic tumor cells will enhance the efficacy of PARPi therapy. Citation Format: Manal Mehibel, Jimmy Xu, Grace Li, Jung Moon, Kaushik Thakkar, Anh Diep, Ryan Kim, Joshua Bloomstein, Siren Xiao, Julien Bacal, Joshua Saldivar, Quynh Le, Karlene Cimprich, Erinn Rankin, Amato Giaccia. Oxygen dependent resistance to PARP inhibitors [abstract]. In: Proceedings of the AACR Virtual Special Conference on Radiation Science and Medicine; 2021 Mar 2-3. Philadelphia (PA): AACR; Clin Cancer Res 2021;27(8_Suppl):Abstract nr IA-003.
科研通智能强力驱动
Strongly Powered by AbleSci AI