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Protein degradation through covalent inhibitor-based PROTACs.
Chemical Communications ( IF 4.9 ) Pub Date : 2020-01-10 , DOI: 10.1039/c9cc08238g Gang Xue 1 , Jiahui Chen , Lihong Liu , Danli Zhou , Yingying Zuo , Tiancheng Fu , Zhengying Pan
Chemical Communications ( IF 4.9 ) Pub Date : 2020-01-10 , DOI: 10.1039/c9cc08238g Gang Xue 1 , Jiahui Chen , Lihong Liu , Danli Zhou , Yingying Zuo , Tiancheng Fu , Zhengying Pan
Affiliation
Tremendous advancements in proteolysis targeting chimera (PROTAC) technology have been made in recent years. However, whether a covalent inhibitor-based PROTAC can be developed remains controversial. Here, we successfully developed chimeric degraders based on covalent inhibitors to degrade BTK and BLK kinases, demonstrating that covalent inhibitor-based PROTACs are viable and useful tools.
中文翻译:
通过基于共价抑制剂的PROTAC降解蛋白质。
近年来,针对嵌合体的蛋白水解(PROTAC)技术取得了巨大的进步。但是,是否可以开发基于共价抑制剂的PROTAC仍存在争议。在这里,我们成功开发了基于共价抑制剂的嵌合降解物,以降解BTK和BLK激酶,证明基于共价抑制剂的PROTAC是可行和有用的工具。
更新日期:2020-01-10
中文翻译:
通过基于共价抑制剂的PROTAC降解蛋白质。
近年来,针对嵌合体的蛋白水解(PROTAC)技术取得了巨大的进步。但是,是否可以开发基于共价抑制剂的PROTAC仍存在争议。在这里,我们成功开发了基于共价抑制剂的嵌合降解物,以降解BTK和BLK激酶,证明基于共价抑制剂的PROTAC是可行和有用的工具。