Inhibitors of PARP: Number crunching and structure gazing

PARP 抑制剂:数值运算和结构凝视

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作者:Johannes Rudolph, Karen Jung, Karolin Luger

Abstract

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.

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