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Discovery of a Potent and Selective Degrader for USP7
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2022-06-12 , DOI: 10.1002/anie.202204395
Yuan Pei 1, 2 , Jingfeng Fu 1, 2 , Yunkai Shi 1, 3 , Mengmeng Zhang 1 , Guanghao Luo 1, 2, 3 , Xiaomin Luo 1, 4 , Ning Song 1, 2 , Tian Mi 1, 2 , Yaxi Yang 1, 2, 3 , Jia Li 1, 2, 3, 4, 5 , Yubo Zhou 1, 2, 3, 4, 5 , Bing Zhou 1, 2, 3
Affiliation  

A first-in-class selective USP7 degrader U7D-1 was developed, inducing potent USP7 degradation in different kinds of cell lines. Importantly, this degrader showed notable anti-proliferative activities in mutant p53 cancer cells, with USP7 inhibitor having no activity.

中文翻译:

发现 USP7 的强效选择性降解剂

开发了一流的选择性 USP7 降解剂U7D-1,在不同种类的细胞系中诱导有效的 USP7 降解。重要的是,这种降解剂在突变的 p53 癌细胞中显示出显着的抗增殖活性,而 USP7 抑制剂没有活性。
更新日期:2022-06-12
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