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Lenalidomide-Br (Compound 41) 是一种基于 Lenalidomide 的 E3 泛素连接酶配体。Lenalidomide-Br 可通过 linker 与靶蛋白配体连接,形成 PROTAC 分子,PROTAC 可诱导促癌蛋白发生泛素化降解。
Lenalidomide-Br (Compound 41) is the Lenalidomide-based ligand. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
[1]. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17. [2]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
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