Inhibitors of PARP: Number crunching and structure gazing

Inhibitors of PARP: Number crunching and structure gazing

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 nex...

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Veröffentlicht in:Proceedings of the National Academy of Sciences - PNAS 2022-03, Vol.119 (11), p.e2121979119-e2121979119
Hauptverfasser: Rudolph, Johannes, Jung, Karen, Luger, Karolin
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
Biological Sciences
BRCA1 Protein - genetics
BRCA2 Protein - genetics
Catalytic activity
DNA Repair
Dose-Response Relationship, Drug
Drug Evaluation, Preclinical
Histones
Homologous recombination
Homology
Humans
Inhibitors
Models, Molecular
Molecular Structure
Mutation
Poly(ADP-ribose) polymerase
Poly(ADP-ribose) Polymerase Inhibitors - chemistry
Poly(ADP-ribose) Polymerase Inhibitors - pharmacology
Poly(ADP-ribose) Polymerase Inhibitors - therapeutic use
Poly(ADP-ribose) Polymerases - chemistry
Poly(ADP-ribose) Polymerases - genetics
Poly(ADP-ribose) Polymerases - metabolism
Protein Binding
Protein Interaction Domains and Motifs
Structure-Activity Relationship
Synthetic Lethal Mutations
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Zusammenfassung: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.
ISSN:0027-8424
1091-6490
DOI:10.1073/pnas.2121979119