Semi-synthesis of Ubiquitin-propargylamide for identifying deubiquitinase targeting inhibitors

文献类型: 外文期刊

第一作者: Tan, Xiaodan

作者: Tan, Xiaodan;Bai, Jingsi;Li, Yi-Ming;Tan, Xiaodan;Ding, Shan;Ren, Yujing;Hong, Danning;Mei, Ziqing;Ren, Yujing;Hong, Danning

作者机构:

关键词: Deubiquitinase; Activity-based probe; Ubiquitin-propargylamide; Protein semi-synthesis; Inhibitor identification

期刊名称:CHINESE CHEMICAL LETTERS ( 影响因子:6.779; 五年影响因子:4.558 )

ISSN: 1001-8417

年卷期: 2019 年 30 卷 3 期

页码:

收录情况: SCI

摘要: Ubiquitin-propargylamide (Ub-PA) is one of the most widely used activity-based probe to measure the activity of deubiquitinases (DUBs) and help validate DUBs targeting inhibitors. However, current synthetic route of Ub-PA is cumbersome. In this work, we report a novel semi-synthetic strategy to prepare Ub-PA in large-scale. Biochemical assays prove that semi-synthetic Ub-PA is an effective probe in identifying DUBs targeting inhibitors. (C) 2018 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

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