USP1 deubiquitinates PARP1 to regulate its trapping and PARylation activity

Sci Adv. 2024 Nov 15;10(46):eadp6567. doi: 10.1126/sciadv.adp6567. Epub 2024 Nov 13.

Abstract

PARP inhibitors (PARPi) represent a game-changing treatment for patients with ovarian cancer with tumors deficient for the homologous recombination (HR) pathway treated with platinum (Pt)-based therapy. PARPi exert their cytotoxic effect by both trapping PARP1 on the damaged DNA and by restraining its enzymatic activity (PARylation). How PARP1 is recruited and trapped at the DNA damage sites and how resistance to PARPi could be overcome are still matters of investigation. Here, we described PARP1 as a substrate of the deubiquitinase USP1. At molecular level, USP1 binds PARP1 to remove its K63-linked polyubiquitination and controls PARP1 chromatin trapping and PARylation activity, regulating sensitivity to PARPi. In both Pt/PARPi-sensitive and -resistant cells, USP1/PARP1 combined blockade enhances replicative stress, DNA damage, and cell death. Our work dissected the biological interaction between USP1 and PARP1 and recommended this axis as a promising and powerful therapeutic choice for not only sensitive but also chemoresistant patients with ovarian cancer irrespective of their HR status.

MeSH terms

  • Cell Line, Tumor
  • DNA Damage*
  • Drug Resistance, Neoplasm / drug effects
  • Drug Resistance, Neoplasm / genetics
  • Female
  • Humans
  • Ovarian Neoplasms* / drug therapy
  • Ovarian Neoplasms* / genetics
  • Ovarian Neoplasms* / metabolism
  • Ovarian Neoplasms* / pathology
  • Poly (ADP-Ribose) Polymerase-1* / metabolism
  • Poly ADP Ribosylation
  • Poly(ADP-ribose) Polymerase Inhibitors* / pharmacology
  • Protein Binding
  • Ubiquitin-Specific Proteases* / genetics
  • Ubiquitin-Specific Proteases* / metabolism
  • Ubiquitination*

Substances

  • USP1 protein, human
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Ubiquitin-Specific Proteases
  • PARP1 protein, human