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Inhibitors of PARP: Number crunching and structure gazing.

Rudolph, Johannes; Jung, Karen; Luger, Karolin.

Proc Natl Acad Sci U S A ; 119(11): e2121979119, 2022 03 15.

Article in English | MEDLINE | ID: mdl-35259019

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.

Subject(s)

Poly(ADP-ribose) Polymerase Inhibitors/chemistry , Poly(ADP-ribose) Polymerase Inhibitors/pharmacology , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , BRCA1 Protein/genetics , BRCA2 Protein/genetics , DNA Repair , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Humans , Models, Molecular , Molecular Structure , Mutation , 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

ABSTRACT

Subject(s)

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