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

作     者：Xiaodan Tan Jingsi Bai Shan Ding Yujing Ren Danning Hong Ziqing Mei Yi-Ming Li 

作者机构：School of Biological and Medical Engineering Hefei University of Technology Tsinghua-Peking Center for Life Sciences Ministry of Education Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical BiologyDepartment of Chemistry Tsinghua University Biotechnology Research Institute Chinese Academy of Agricultural Sciences School of Biological Science Beijing Institute of Technology 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2019年第30卷第3期

页      面：743-746页

核心收录：

学科分类：07[理学] 0703[理学-化学] 

基　　金：supported by the National Natural Science Foundation of China(Nos. 91753205 and 21877024 to Y. Li and No. 31640016 to Z. Mei) the Fundamental Research Funds for the Central Universities (No. PA2017GDQT0021 to Y. Li) the funding of National Key R&D program of China(No. 2017YFD0500400 to Z. Mei) the Fundamental Research Funds for the Central Non-profit Scientific Institution (No. Y2016JC25 to Z. Mei) the Agricultural Science and Technology Innovation Program to Z.Mei 

主　　题：Deubiquitinase Activity-based probe Ubiquitin-propargylamide Protein semi-synthesis Inhibitor identification 

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.