基于微管蛋白的双靶点化合物和蛋白质降解剂用于癌症治疗-最新综述（2021年至今）

IF 5.9 2区医学 Q1 CHEMISTRY, MEDICINAL

European Journal of Medicinal Chemistry Pub Date : 2025-09-24 DOI:10.1016/j.ejmech.2025.118191

Shijia Li, Zhouyan Liu, Tong Li, Ziwei Tang, Yanyan Feng, Cheng Chen, Chenglei Gu, Jichao Chen

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引用次数: 0

摘要

同时调节微管动力学和其他致癌靶标活性已被证明是对抗癌症的可行方法。在过去的几十年里，许多基于微管蛋白的双靶点化合物已经成功地开发出来，具有增强抗肿瘤疗效、克服耐药和减少副作用的能力。本文综述了近五年来基于微管蛋白的双靶点化合物的最新进展，重点介绍了它们的靶点选择、设计策略、构效关系分析和抗癌特性。此外，还综述了基于微管蛋白聚合抑制剂的新型靶向蛋白降解剂。此外，还提出了基于微管蛋白的双靶点化合物未来发展可能面临的挑战和相应的补救措施。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Tubulin-based dual-target compounds and protein degraders for cancer therapy—An updated review (2021-present)

查看原文本刊更多论文

Tubulin-based dual-target compounds and protein degraders for cancer therapy—An updated review (2021-present)

Simultaneous regulation of microtubule dynamics and other carcinogenic target activity has been proven a viable approach to combat cancer. Over the past few decades, numerous tubulin-based dual-target compounds have successfully been developed with the capacity to enhance antitumor efficacy and surmount drug resistance as well as reduce side effects. This review provides an updated overview of tubulin-based dual-target compounds in the recent five years, emphasizing their target selection, design strategy, structure-activity relationship analysis, and anticancer properties. Moreover, emerging targeted protein degraders based on tubulin polymerization inhibitors are also summarized. Additionally, potential challenges and the corresponding remedies are proposed for the future development of tubulin-based dual-target compounds.

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来源期刊

European Journal of Medicinal Chemistry 化学-医药化学

CiteScore

11.70

自引率

9.00%

发文量

863

审稿时长

29 days

期刊介绍： The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.