奥拉帕利
Olaparib.
作者信息
Goulooze S C, Cohen A F, Rissmann R
机构信息
Centre for Human Drug Research, Leiden, the Netherlands.
Leiden University Medical Center, Leiden, the Netherlands.
出版信息
Br J Clin Pharmacol. 2016 Jan;81(1):171-3. doi: 10.1111/bcp.12761. Epub 2015 Oct 24.
Abstract
Olaparib is used to treat BReast CAncer susceptibility protein (BRCA)-associated, platinum-sensitive ovarian cancer. Olaparib inhibits poly(ADP-ribose) polymerase, thereby blocking the repair of single-strand DNA breaks. This results in synthetic lethality in BRCA-associated cancer cells, which have a dysfunction of another DNA repair pathway - homologous recombination.
摘要
奥拉帕利用于治疗与乳腺癌易感蛋白（BRCA）相关的铂敏感型卵巢癌。奥拉帕利可抑制聚（ADP - 核糖）聚合酶，从而阻断单链DNA断裂的修复。这在BRCA相关癌细胞中导致合成致死，这些癌细胞存在另一种DNA修复途径——同源重组功能障碍。
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本文引用的文献
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Error-Prone Repair of DNA Double-Strand Breaks.DNA双链断裂的易错修复
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PARP inhibitors in BRCA mutation-associated ovarian cancer.PARP抑制剂在BRCA突变相关的卵巢癌中的应用
Lancet Oncol. 2015 Jan;16(1):10-2. doi: 10.1016/S1470-2045(14)71172-6. Epub 2014 Dec 4.
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Olaparib maintenance therapy in patients with platinum-sensitive relapsed serous ovarian cancer: a preplanned retrospective analysis of outcomes by BRCA status in a randomised phase 2 trial.奥拉帕利维持治疗铂类敏感复发性卵巢浆液性癌患者：随机 2 期试验中 BRCA 状态的预设回顾性分析结果
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The role of PARP in DNA repair and its therapeutic exploitation.PARP 在 DNA 修复中的作用及其治疗性开发。
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Poly(ADP)-ribose polymerase inhibition: frequent durable responses in BRCA carrier ovarian cancer correlating with platinum-free interval.聚（ADP-核糖）聚合酶抑制：BRCA 携带者卵巢癌中频繁的持久缓解与铂类无进展间期相关。
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