Inhibitors of PARP: Number crunching and structure gazing
Johannes Rudolph, Karen Jung, Karolin Luger
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.
Topics & Concepts
Poly ADP ribose polymeraseComputer scienceComputational biologyBiologyGeneticsDNAPolymerasePARP inhibition in cancer therapyCell death mechanisms and regulationIntegrated Circuits and Semiconductor Failure Analysis