Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment,Journal of Medicinal Chemistry

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Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2022-12-13 , DOI: 10.1021/acs.jmedchem.2c01352
Jie Zhang ₁ , Yuqi Gao _{2,

3} , Zipeng Zhang ₃ , Jinbo Zhao _{1,

4} , Wenshuang Jia ₃ , Chengcai Xia ₁ , Fugang Wang ₅ , Tingting Liu ₁

Affiliation

The nuclear enzymes called poly(ADP-ribose)polymerases (PARPs) are known to catalyze the process of PARylation, which plays a vital role in various cellular functions. They have become important targets for the discovery of novel antitumor drugs since their inhibition can induce significant lethality in tumor cells. Therefore, researchers all over the world have been focusing on developing novel and potent PARP inhibitors for cancer therapy. Studies have shown that PARP inhibitors and other antitumor agents, such as EZH2 and EGFR inhibitors, play a synergistic role in cancer cells. The combined inhibition of PARP and the targets with synergistic effects may provide a rational strategy to improve the effectiveness of current anticancer regimens. In this Perspective, we sum up the recent advance of PARP-targeted agents, including single-target inhibitors/degraders and dual-target inhibitors/degraders, discuss the fundamental theory of developing these dual-target agents, and give insight into the corresponding structure–activity relationships of these agents.

中文翻译：

基于 PARP 抑制的多疗法：癌症治疗的潜在治疗方法

已知称为聚（ADP-核糖）聚合酶 (PARP) 的核酶可催化 PARylation 过程，该过程在各种细胞功能中起着至关重要的作用。它们已成为发现新型抗肿瘤药物的重要靶标，因为它们的抑制作用可以在肿瘤细胞中引起显着的杀伤力。因此，世界各地的研究人员一直致力于开发用于癌症治疗的新型强效 PARP 抑制剂。研究表明，PARP 抑制剂和其他抗肿瘤药物，如 EZH2 和 EGFR 抑制剂，在癌细胞中发挥协同作用。联合抑制 PARP 和具有协同作用的靶点可能为提高当前抗癌方案的有效性提供合理的策略。在此观点中，我们总结了 PARP 靶向药物的最新进展，

更新日期：2022-12-13

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