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.
Keywords:
HPF1; cancer drugs; drug specificity; inhibitor of Parp; synthetic lethality.
MeSH terms
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use
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BRCA1 Protein / genetics
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BRCA2 Protein / genetics
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DNA Repair
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Dose-Response Relationship, Drug
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Drug Evaluation, Preclinical
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Humans
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Models, Molecular
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Molecular Structure
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Mutation
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Poly(ADP-ribose) Polymerase Inhibitors / chemistry*
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Poly(ADP-ribose) Polymerase Inhibitors / pharmacology*
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Poly(ADP-ribose) Polymerase Inhibitors / therapeutic use
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Poly(ADP-ribose) Polymerases / chemistry
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Poly(ADP-ribose) Polymerases / genetics
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Poly(ADP-ribose) Polymerases / metabolism
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Protein Binding
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Protein Interaction Domains and Motifs
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Structure-Activity Relationship
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Synthetic Lethal Mutations
Substances
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Antineoplastic Agents
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BRCA1 Protein
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BRCA2 Protein
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Poly(ADP-ribose) Polymerase Inhibitors
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Poly(ADP-ribose) Polymerases