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Development of Selective PARP1 Inhibitors for Treatment of Cancer

Xin Zhou1, Steven H Liang1

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

ACS Medicinal Chemistry Letters
|October 15, 2025
PubMed

Insights

New compounds show high selectivity for Poly-(ADP-ribose) polymerase 1 (PARP1) over PARP2. This targeted approach is crucial for developing safer, next-generation cancer therapeutics with fewer side effects.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Poly-(ADP-ribose) polymerase 1 (PARP1) is a key enzyme in DNA damage response.
  • Inhibiting PARP enzymes is a strategy for cancer therapy.
  • Current inhibitors may affect multiple PARP subtypes, leading to adverse effects.

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