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Dual-target inhibitors based on PARP1: new trend in the development of anticancer research

Jun Ge1, Yu Yin1, Yingpeng Li1

  • 1School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China.

Future Medicinal Chemistry
|March 8, 2022
PubMed

Insights

Dual-target inhibitors based on Poly (ADP-ribose) polymerase 1 (PARP1) offer improved cancer therapy by overcoming limitations of single-target drugs. This review explores their design and potential.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Poly (ADP-ribose) polymerase 1 (PARP1) inhibitors are approved cancer therapeutics.
  • Limitations include drug resistance, side effects, and low efficiency.
  • Dual-target drugs offer synergistic effects for multifactorial diseases.

Purpose of the Study:

  • To review research progress on dual-target inhibitors based on PARP1.
  • To discuss drug design strategies and structure-activity relationships for these inhibitors.

Main Methods:

  • Literature review of dual-target PARP1 inhibitors.
  • Analysis of drug design principles.
  • Examination of structure-activity relationships.

Main Results:

  • Several dual-target PARP1 inhibitors have shown unique advantages.
  • Dual-targeting strategies aim to enhance efficacy and reduce resistance.
  • Specific design approaches and SAR data are emerging.

Conclusions:

  • Dual-target PARP1 inhibitors represent a promising approach for cancer therapy.
  • Further research into design strategies and SAR is crucial.
  • This work provides references for developing next-generation PARP1 inhibitors.
Keywords:
BRCAnessPARP1PARP1 inhibitoranti-cancer drugdual-target inhibitorstructure–activity relationship

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