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PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention

Xiaolei Zhu, Xiaodong Ma, Yongzhou Hu1

  • 1ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.. huyz@zju.edu.cn.

Current Medicinal Chemistry
|September 24, 2014
PubMed

Insights

Poly(ADP-ribose) polymerase 1 (PARP1) inhibitors show promise in cancer treatment by enhancing chemotherapy and targeting cancer cells with DNA repair defects. This review categorizes 12 PARP1 inhibitors in clinical trials by chemical structure.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Poly(ADP-ribose) polymerase 1 (PARP1) plays a crucial role in DNA repair, making it a significant target for cancer therapy.
  • PARP1 inhibition enhances chemosensitization and antiproliferation in cancer cells with defective homologous recombination.
  • The development of PARP1 inhibitors offers a novel therapeutic strategy for oncology.

Purpose of the Study:

  • To provide a comprehensive overview of currently investigated PARP1 inhibitors in clinical trials.
  • To classify PARP1 inhibitors based on their chemical structures.
  • To highlight the potential for future development of PARP1-targeted anticancer therapeutics.

Main Methods:

  • Literature review and classification of PARP1 inhibitors based on chemical structure.
  • Categorization into lactam type, pseudo ring type, and untypical PARP1 inhibitors.
  • Analysis of 12 PARP1 inhibitors that have advanced into clinical trials.

Main Results:

  • Twelve PARP1 inhibitors have been developed and entered clinical trials.
  • The inhibitors are classified into three main structural categories: lactam, pseudo ring, and untypical.
  • This classification provides a structured overview of the current landscape of PARP1 inhibitor development.

Conclusions:

  • PARP1 inhibitors represent a promising class of anticancer agents.
  • Structural classification aids in understanding the diversity and development trajectory of PARP1 inhibitors.
  • Further exploration of these candidates can inform the design of next-generation PARP1-targeted therapies.

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