Open AccessInhibitors of PARP: Number crunching and structure gazing
Author(s) -
Johannes Rudolph,
Karen Jung,
Karolin Luger
Publication year - 2022
Publication title -
proceedings of the national academy of sciences of the united states of america
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.011
H-Index - 771
eISSN - 1091-6490
pISSN - 0027-8424
DOI - 10.1073/pnas.2121979119
Subject(s) - synthetic lethality , homologous recombination , prostate cancer , in vivo , poly adp ribose polymerase , parp inhibitor , breast cancer , cancer , olaparib , computational biology , cancer research , ovarian cancer , in vitro , biology , dna repair , bioinformatics , medicine , genetics , dna , polymerase
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.