文献类型：期刊文献

英文题名：A carbapenem-based fluorescence assay for the screening of metallo-β-lactamase inhibitors

作者：Qian, Xiana[1];Zhang, Shuangzhan[1];Xue, Shuyuan[1];Mao, Wuyu[1];Xu, Minqiu[1];Xu, Weipan[1];Xie, Hexin[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, State Key Lab Bioreactor Engn, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China

年份：2019

卷号：29

期号：2

起止页码：322

外文期刊名：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000454616600038)】；

基金：We are extremely grateful for financial support from the National Natural Science Foundation of China (21472048), the "Thousand Plan" Youth Program, and the Fundamental Research Funds for the Central Universities.

语种：英文

外文关键词：Metallo-beta-lactamase; Fluorescence; Screening assay; Inhibitor

摘要：Reported herein is a fluorescence assay for the rapid screening of metallo-beta-lactamase (MBL) inhibitors. This assay employs a fluorogenic carbapenem CPC-1 as substrate and is compatible with all MBLs, including B1, B2 and B3 subclass MBLs. The efficiency of this assay was demonstrated by the rapid inhibition screening of a number of molecules against B2 MBL CphA and 2,3-dimercaprol was identified as a potent CphA inhibitor.