一种笼状 E3 连接酶配体，用于 PROTAC 介导的光控蛋白降解。
A caged E3 ligase ligand for PROTAC-mediated protein degradation with light.
机构信息
Department of Chemistry, Imperial College London, Molecular Sciences Research Hub, White City Campus, Wood Lane, London W12 0BZ, UK.
Cellzome GmbH, a GSK Company, Meyerhofstrasse 1, 69117 Heidelberg, Germany.
出版信息
Chem Commun (Camb). 2020 May 21;56(41):5532-5535. doi: 10.1039/d0cc00523a. Epub 2020 Apr 16.
With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy.
为了实现 PROTAC 诱导的蛋白质降解在更大时空范围内的控制，通过光笼蔽 BRD4 靶向 PROTAC 中必需的 E3 连接酶结合基序来设计光激活降解剂。只有在短时间的辐照后才会触发蛋白水解，其动力学可以通过活细胞视频显微镜进行监测。
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