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2022年对PROTAC降解剂作为抗癌剂的年度审查

Xiao Wang¹, Zhao-Long Qin², Na Li²

¹School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, China.

European journal of medicinal chemistry

|January 28, 2024

概括

蛋白质溶解向嵌合体 (PROTAC) 技术显示出显著的进步,到2022年,超过20种药物正在临床试验中. 针对KRAS^G12C,BRD4和其他关键蛋白质的新型PROTAC显示出作为新型抗癌剂的前景.

科学领域:

生物化学生物化学
药用化学医学化学
在瘤学瘤学.

背景情况:

在过去二十年中,蛋白质溶解向嵌合体 (PROTAC) 技术取得了显著的进步.
到2022年底,超过20种PROTAC药物进入临床试验,其中ARV-471 (ER向) 处于III期.

研究的目的:

根据2022年的出版物,审查和更新PROTAC降解剂作为潜在抗癌剂的地位.
突出设计策略,降解效应和新型PROTACs的抗癌活动.

主要方法:

2022年发表的科学文章的文献综述,重点关注 PROTAC 技术及其抗癌应用.
对PROTAC降解剂的设计策略,降解效率和临床前/临床结果的分析.

主要成果:

为KRAS^G12C开发了第一个可逆共价降解剂.
获得了HDCA1降解剂的亚微分子活性,并发现了一种新的FEM1B配体 (EN106).
报告了第一个针对SOS1,BRD4异型 (BRD4 L/S) 的PROTAC,以及对CDK9/Cyclin T1.1的双降解剂.

结论:

PROTAC技术继续产生有前途的抗癌药物候选药物,具有不同的向特异性.
在2022年,近期的进展为开发有效的基于PROTAC的癌症疗法提供了新的策略和工具,这些疗法具有改进的类似药物的特性.

关键词:

抗癌活动抗癌活动降解降解是一种降解.这就是PROTAC.这就是为什么UPSUPSUPSUPS.

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