基于碳青霉烯的荧光分析法用于筛选金属β-内酰胺酶抑制剂。
A carbapenem-based fluorescence assay for the screening of metallo-β-lactamase inhibitors.
机构信息
State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
出版信息
Bioorg Med Chem Lett. 2019 Jan 15;29(2):322-325. doi: 10.1016/j.bmcl.2018.11.025. Epub 2018 Nov 13.
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.
本文报道了一种用于快速筛选金属β-内酰胺酶（MBL）抑制剂的荧光检测法。该方法以荧光碳青霉烯类化合物 CPC-1 为底物，适用于所有 MBL，包括 B1、B2 和 B3 亚类 MBL。通过快速抑制筛选 B2 MBL CphA 对多种分子的效率，证明了该方法的有效性，2,3-二巯基丙醇被鉴定为 CphA 的有效抑制剂。
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