Tackling PARP inhibitor resistance

Trends Cancer. 2021 Dec;7(12):1102-1118. doi: 10.1016/j.trecan.2021.08.007. Epub 2021 Sep 22.

Abstract

Homologous recombination-deficient (HRD) tumours, including those harbouring mutations in the BRCA genes, are hypersensitive to treatment with inhibitors of poly(ADP-ribose) polymerase (PARPis). Despite high response rates, most HRD cancers ultimately develop resistance to PARPi treatment through reversion mutations or genetic/epigenetic alterations to DNA repair pathways. Counteracting these resistance pathways, thereby increasing the potency of PARPi therapy, represents a potential strategy to improve the treatment of HRD cancers. In this review, we discuss recent insights derived from genetic screens that have identified a number of novel genes that can be targeted to improve PARPi treatment of HRD cancers and may provide a means to overcome PARPi resistance.

Keywords: base excision repair; homologous recombination repair; nucleotide metabolism; poly(ADP-ribose) polymerase inhibitors; therapy resistance.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / therapeutic use
  • Drug Resistance, Neoplasm
  • Female
  • Genes, Tumor Suppressor
  • Homologous Recombination / genetics
  • Humans
  • Ovarian Neoplasms* / drug therapy
  • Poly(ADP-ribose) Polymerase Inhibitors / pharmacology
  • Poly(ADP-ribose) Polymerase Inhibitors / therapeutic use

Substances

  • Antineoplastic Agents
  • Poly(ADP-ribose) Polymerase Inhibitors