European journal of medicinal chemistry · 2025
Tubulin-based dual-target compounds and protein degraders for cancer therapy-An updated review (2021-present).
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Li Shijia, Liu Zhouyan, Li Tong, Tang Ziwei, Feng Yanyan, Chen Cheng, Gu Chenglei, Chen Jichao
Аннотация
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.