Inhibitors of PARP: Number crunching and structure gazing.

Rudolph, Johannes; Jung, Karen; Luger, Karolin · Proc Natl Acad Sci U S A · 2022

review · Level V

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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<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.

Medical subject headings