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Poly(ADP-Ribose) Polymerase (PARP) Inhibitors for Cancer Therapy: Advances, Challenges, and Future Directions

Denys Bondar1, Yevgen Karpichev1

  • 1Department of Chemistry and Biotechnology, Tallinn University of Technology (TalTech), Akadeemia tee 15, 12618 Tallinn, Estonia.

Biomolecules
|October 26, 2024
PubMed

Insights

Poly(ADP-ribose) polymerases (PARPs) are key proteins in DNA repair and cancer. PARP inhibitors show promise as anticancer drugs, with new generations offering improved efficacy and synthesis methods.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Poly(ADP-ribose) polymerases (PARPs) are vital nuclear proteins involved in DNA repair, transcription, and cell death.
  • PARP1, the most abundant PARP, functions as a DNA damage sensor and is a significant target in cancer therapy.
  • Elevated PARP expression in tumors like melanoma, lung, and breast cancer correlates with poor prognosis and treatment resistance.

Purpose of the Study:

  • To review the properties, development, and therapeutic mechanisms of PARP inhibitors.
  • To discuss advancements from first-generation to third-generation PARP inhibitors.
  • To explore sustainable synthesis methods and green chemistry approaches for novel anticancer agents.

Main Methods:

  • Literature review of PARP inhibitors' properties and development.
  • Analysis of therapeutic mechanisms and potential off-target applications.
  • Discussion of synthesis strategies, including green chemistry.

Main Results:

  • PARP inhibitors, particularly third-generation compounds, demonstrate efficacy as monotherapies and in combination with chemo- and radiotherapy.
  • Ongoing Phase II clinical trials highlight the therapeutic potential of advanced PARP inhibitors.
  • Sustainable synthesis methods are crucial for discovering new anticancer agents targeting PARP.

Conclusions:

  • PARP inhibitors represent a promising class of anticancer agents with evolving therapeutic strategies.
  • Further research into novel synthesis methods and targeting strategies can enhance their clinical utility.
  • Green chemistry principles offer sustainable pathways for developing next-generation PARP-targeted cancer therapies.
Keywords:
PARP inhibitorsanticancer agentspoly(ADP-ribose) polymerase

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