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The Promise of Selective PARP1 Inhibitors in Cancer Therapy

Xin Zhou1, Jimmy S Patel1, Taoqian Zhao1

  • 1Department of Radiology and Imaging Sciences, Emory University, 1364 Clifton Road, Atlanta, Georgia 30322, United States.

ACS Medicinal Chemistry Letters
|November 19, 2025
PubMed

Insights

Poly-(ADP-ribose) polymerase 1 (PARP1) is key in DNA repair. A new selective PARP1 inhibitor, (S)-G9, shows promise for cancer therapy, especially in tumors with homologous recombination deficiencies (HRDs).

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Poly-(ADP-ribose) polymerase 1 (PARP1) is a crucial enzyme in cellular DNA damage response pathways.
  • PARP1 inhibition is a validated therapeutic strategy, particularly effective in cancers exhibiting homologous recombination deficiencies (HRDs).

Purpose of the Study:

  • To report the discovery and characterization of a novel, selective inhibitor of PARP1.
  • To present (S)-G9 as a potential candidate for clinical development in oncology.

Main Methods:

  • Enzyme inhibition assays to determine selectivity and potency.
  • Cellular assays to assess DNA damage response modulation.
  • In vivo studies to evaluate anti-tumor efficacy (details not provided in abstract).

Main Results:

  • Identification of (S)-G9 as a potent and selective inhibitor of PARP1.
  • Demonstration of (S)-G9's potential as a therapeutic agent (specific results not detailed in abstract).

Conclusions:

  • The discovery of (S)-G9 represents a significant advancement in the development of targeted cancer therapies.
  • (S)-G9 is a promising PARP1 inhibitor poised for further clinical investigation.
Keywords:
DNA damage response; homologous recombination deficiency (HRD)Poly(ADP-ribose) polymerase 1 (PARP1)Poly(ADP-ribose) polymerase inhibitor (PARPi)anticancerstructure−activity relationship (SAR)

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