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Published on: November 9, 2020
Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation
Haixia Liu1,2, Chaowei Ren1,3, Renhong Sun1
1Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai, 201210, China. chenhl@shanghaitech.edu.cn.
Abstract:
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.
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