PARP Inhibitors for Cancer Therapy

Cell. 2017 Apr 6;169(2):183. doi: 10.1016/j.cell.2017.03.034.

Abstract

Rucaparib is an inhibitor of nuclear poly (ADP-ribose) polymerases (inhibition of PARP-1 > PARP-2 > PARP-3), following a similar drug, Olaparib. It disrupts DNA repair and replication pathways (and possibly transcription), leading to selective killing of cancer cells with BRCA1/2 mutations. Rucaparib is approved for recurrent ovarian cancers with germline or somatic mutations in BRCA1/2.

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • BRCA1 Protein / genetics
  • BRCA2 Protein / genetics
  • Drug Approval
  • Female
  • Humans
  • Indoles / therapeutic use*
  • Mutation
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / genetics
  • Poly(ADP-ribose) Polymerase Inhibitors / therapeutic use*

Substances

  • Antineoplastic Agents
  • BRCA1 Protein
  • BRCA1 protein, human
  • BRCA2 Protein
  • BRCA2 protein, human
  • Indoles
  • Poly(ADP-ribose) Polymerase Inhibitors
  • rucaparib