PARP7：一个新兴的治疗靶点——对生物功能的见解和小分子抑制剂开发的进展

IF 6.8 1区医学 Q1 CHEMISTRY, MEDICINAL

Journal of Medicinal Chemistry Pub Date : 2025-09-24 DOI:10.1021/acs.jmedchem.5c01335

Feihuang Qiu, Jianqiao Wang, Kehan Huang, Tianxiang Shang, Chenghao Wang, Wenxin Yan, Yungen Xu, Hongfeng Gu

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引用次数: 0

摘要

PARP7是PARP家族中一个至关重要的成员。目前的研究表明，PARP7与多种疾病有关，包括病毒感染、癌症和中风。因此，PARP7酶活性的药理学调节已成为治疗许多疾病的关键策略。值得注意的是，用于肿瘤治疗的选择性PARP7抑制剂RBN-2397已进入II期试验，突出了靶向该酶的翻译潜力。本文就PARP7的生物学功能及其在多种疾病中的作用进行综述。此外，为了推进PARP7抑制剂的研究，我们分析了现有论文和专利中报道的PARP7抑制剂的作用机制和设计策略。此外，我们还分享了我们在PARP7抑制剂设计方面的经验，并就这一开创性研究领域的机遇和挑战提出了我们的见解。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

PARP7: an Emerging Therapeutic Target-Insights into Biological Functions and Advances in Small-Molecule Inhibitor Development

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PARP7: an Emerging Therapeutic Target-Insights into Biological Functions and Advances in Small-Molecule Inhibitor Development

PARP7 is a critically important member of the PARP family. Current research indicates that PARP7 is associated with various diseases, including viral infections, cancers, and stroke. Consequently, pharmacological modulation of PARP7 enzymatic activity has emerged as a crucial strategy for treating numerous diseases. Notably, the selective PARP7 inhibitor RBN-2397 for tumor treatment has entered Phase II trials, highlighting the translational potential of targeting this enzyme. This perspective summarizes the biological functions of PARP7 and its roles in various diseases. Furthermore, to advance the study of PARP7 inhibitors, we analyze the mechanisms of action and design strategies of existing PARP7 inhibitors as reported in current papers and patents. Additionally, we share our experiences in designing PARP7 inhibitors and present our insights regarding the opportunities and challenges in this pioneering research field.

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来源期刊

Journal of Medicinal Chemistry 医学-医药化学

CiteScore

4.00

自引率

11.00%

发文量

804

审稿时长

1.9 months

期刊介绍： The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents. The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.