PARP 抑制剂：数字运算与结构观察。
Inhibitors of PARP: Number crunching and structure gazing.
机构信息
Department of Biochemistry, University of Colorado Boulder, Boulder, CO 80309.
HHMI, University of Colorado Boulder, Boulder, CO 80309.
出版信息
Proc Natl Acad Sci U S A. 2022 Mar 15;119(11):e2121979119. doi: 10.1073/pnas.2121979119. Epub 2022 Mar 8.
SignificancePARP is an important target in the treatment of cancers, particularly in patients with breast, ovarian, or prostate cancer that have compromised homologous recombination repair (i.e., BRCA). This review about inhibitors of PARP (PARPi) is for readers interested in the development of next-generation drugs for the treatment of cancer, providing insights into structure-activity relationships, in vitro vs. in vivo potency, PARP trapping, and synthetic lethality.
聚腺苷二磷酸核糖聚合酶（PARP）是癌症治疗的一个重要靶点，尤其是在同源重组修复（HRR）功能缺陷的乳腺癌、卵巢癌或前列腺癌患者中（例如 BRCA 缺陷）。本文综述了聚腺苷二磷酸核糖聚合酶抑制剂（PARPi），旨在为关注下一代癌症治疗药物研发的读者提供 PARP 抑制剂的结构-活性关系、体外与体内药效、PARP 捕获和合成致死等方面的深入见解。
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