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荧光偏振和各向异性法研究β-内酰胺类抗菌药物、β-内酰胺酶和青霉素结合蛋白:综述。

Investigation of β-lactam antibacterial drugs, β-lactamases, and penicillin-binding proteins with fluorescence polarization and anisotropy: a review.

机构信息

Entasis Therapeutics, 35 Gatehouse Drive, Waltham, MA 02451, USA.

出版信息

Methods Appl Fluoresc. 2016 Apr 12;4(2):024002. doi: 10.1088/2050-6120/4/2/024002.

Abstract

This review covers the uses of fluorescence polarization and anisotropy for the investigation of bacterial penicillin binding proteins (PBPs), which are the targets of β-lactam antibacterial drugs (penicillins, cephalosporins, carbapenems, and monobactams), and of the β-lactamase enzymes that destroy these drugs and help to render bacterial pathogens resistant to them. Fluorescence polarization and anisotropy-based methods for quantitation of β-lactam drugs are also reviewed. A particular emphasis is on methods for quantitative measurement of the interactions of β-lactams and other inhibitors with PBPs and β-lactamases.

摘要

这篇综述涵盖了荧光偏振和各向异性在研究细菌青霉素结合蛋白(PBPs)中的应用,这些蛋白是β-内酰胺类抗菌药物(青霉素、头孢菌素、碳青霉烯类和单环β-内酰胺类)的靶标,也是破坏这些药物并帮助使细菌病原体对其产生耐药性的β-内酰胺酶的靶标。本文还回顾了基于荧光偏振和各向异性的定量检测β-内酰胺类药物的方法。特别强调的是定量测量β-内酰胺类药物和其他抑制剂与 PBPs 和β-内酰胺酶相互作用的方法。

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