响应活性氧物种的前 PROTAC 用于肿瘤特异性蛋白质降解。
Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation.
机构信息
Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai, 201210, China.
School of Physical Science and Technology, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai, 201210, China.
出版信息
Chem Commun (Camb). 2022 Sep 8;58(72):10072-10075. doi: 10.1039/d2cc03367d.
By introducing a reactive oxygen species (ROS) triggered leaving group (arylboronic acid) to the parent PROTACs, ROS-responsive Pre-PROTACs were designed and evaluated. Pre-PROTAC (7) efficiently degraded the target protein BRD3 according to ROS levels. Our research provides an effective approach to control PROTAC activation by the endogenous ROS-related microenvironment.
通过在母型 PROTAC 中引入一个活性氧（ROS）触发的离去基团（芳基硼酸），设计并评估了 ROS 响应性的前体 PROTAC。根据 ROS 水平，前体 PROTAC（7）有效地降解了靶蛋白 BRD3。我们的研究为通过内源性 ROS 相关的微环境控制 PROTAC 的激活提供了一种有效的方法。
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