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A carbapenem-based fluorescence assay for the screening of metallo-β-lactamase inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-11-13 , DOI: 10.1016/j.bmcl.2018.11.025
Xiana Qian , Shuangzhan Zhang , Shuyuan Xue , Wuyu Mao , Minqiu Xu , Weipan Xu , Hexin Xie

Reported herein is a fluorescence assay for the rapid screening of metallo-β-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.



中文翻译:

基于碳青霉烯的荧光测定法筛选金属β-内酰胺酶抑制剂

本文报道了用于快速筛选金属-β-内酰胺酶(MBL)抑制剂的荧光测定法。该测定法采用荧光碳青霉烯CPC-1作为底物,并且与所有MBL(包括B1,B2和B3亚类MBL)兼容。通过对B2 MBL CphA的许多分子进行快速抑制筛选,证明了该测定的效率,并确定了2,3-二聚己醇为有效的CphA抑制剂。

更新日期:2018-11-13
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