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Recent advances in structural types and medicinal chemistry of PARP-1 inhibitors

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Abstract

Poly (ADP-ribose) Polymerase-1 (PARP-1) is a member of 17 membered PARP family having diversified biological functions such as synthetic lethality, DNA repair, apoptosis, necrosis and histone binding, etc. The U.S. FDA has approved four PARP-1 inhibitors, namely Olaparib, Rucaparib, Niraparib, and Talazoparib. And, Veliparib has entered the late stage of clinical research as a PARP-1 inhibitor. At present, PARP-1 inhibitors have been approved for ovarian cancer, breast cancer, pancreatic cancer and other related indications. In recent years, more and more novel PARP-1 inhibitors have been reported. This review has attempted to summarize the structural types and characteristics of various novel PARP-1 inhibitors reported since 2020. And we outlined the current clinical application potential of PARP-1 inhibitors and further analyzed its current challenges and future development trends.

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Acknowledgements

This work was funded by Science and Technology Project of Hebei Education Department (NO. QN2022161), and the 2022 Research Start‐up Fund for High‐level Talents of Chengde Medical University (NO. 202207).

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Authors and Affiliations

  1. Department of Pharmacy, Anorectal Hospital of Chengde Medical University, Chengde, 067000, P. R. China

    Ling Yu

  2. Key Laboratory of Traditional Chinese Medicine Research and Development of Hebei Province, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, 067000, P. R. China

    Zhi-wei Yan, You-de Wang, Jing-yi Zhao & Shuai Li

  3. School of basic medical sciences, Chengde Medical University, Chengde, 067000, P. R. China

    Hao Miao & Chong Pang

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Yu, L., Yan, Zw., Wang, Yd. et al. Recent advances in structural types and medicinal chemistry of PARP-1 inhibitors. Med Chem Res 31, 1265–1276 (2022). https://doi.org/10.1007/s00044-022-02919-6

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