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 

机构地区：[1]School of Biological and Medical Engineering, Hefei University of Technology [2]Tsinghua-Peking Center for Life Sciences, Ministry of Education Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology,Department of Chemistry, Tsinghua University [3]Biotechnology Research Institute, Chinese Academy of Agricultural Sciences [4]School of Biological Science, Beijing Institute of Technology

出　　处：《Chinese Chemical Letters》2019年第3期743-746,共4页中国化学快报（英文版）

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

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.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.

关 键 词：Deubiquitinase Activity-based probe Ubiquitin-propargylamide Protein SEMI-SYNTHESIS INHIBITOR identification 

分 类 号：O6[理学—化学]