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Inhibitors of PARP: Number crunching and structure gazing

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Significance PARP 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… Click to show full abstract

Significance PARP 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.

Keywords: parp number; crunching structure; structure gazing; structure; number crunching; inhibitors parp

Journal Title: Proceedings of the National Academy of Sciences of the United States of America
Year Published: 2022

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