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Inhibitors of PARP: Number crunching and structure gazing.


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.

SUBMITTER: Rudolph J 

PROVIDER: S-EPMC8931346 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature

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Inhibitors of PARP: Number crunching and structure gazing.

Rudolph Johannes J   Jung Karen K   Luger Karolin K  

Proceedings of the National Academy of Sciences of the United States of America 20220308 11


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<sup>-/-</sup>). 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. ...[more]

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