Structural and Functional Aspects of Extended-Spectrum AmpC Cephalosporinases

Rachel A. Powers

doi:10.2174/1573399811666150615144707

摘要

Β-内酰胺类抗生素已经彻底改变了现代医学，但这些药物的耐药性也成为了一个重大的公共卫生危机。传统上，C类β-内酰胺酶被称为头孢菌素酶，由于其酶作用物更青睐于这类独特的β内酰胺类。然而，具有广谱活性（广谱头孢菌素或ESACs）的AmpC酶的出现尤其令人担忧，尤其是考虑到大多数临床β内酰胺酶抑制剂对这些酶无效。本文总结了几种广谱C类β内酰胺酶的结构，并分析了所观察到的它们之间的构效关系。

关键词: Β-内酰胺酶；头孢菌素；广谱；构效；X射线晶体结构

« Previous Next »

图形摘要

Rights & Permissions Print Cite

Current Drug Targets

Title:Structural and Functional Aspects of Extended-Spectrum AmpC Cephalosporinases

Volume: 17 Issue: 9

Author(s): Rachel A. Powers

Affiliation:

关键词: Β-内酰胺酶；头孢菌素；广谱；构效；X射线晶体结构

摘要: β-lactam antibiotics have revolutionized modern medicine, but resistance to these drugs is a major public health crisis. Traditionally, class C β-lactamases were referred to as cephalosporinases due to their substrate preference for this particular class of β-lactams. However, the emergence of AmpC enzymes with extended-spectrum activity (extended-spectrum cephalosporinases or ESACs) is particularly worrisome, especially given that most clinical β-lactamase inhibitors are ineffective against these enzymes. This review summarizes structures of several extended spectrum class C β-lactamases and analyzes the structure-function relationship observed among them.

Export Options

Export File:

RIS (for EndNote, Reference Manager, ProCite)

BibTeX

Text

Content:

Citation Only

Citation and Abstract

About this article

Cite this article as:

Rachel A. Powers , Structural and Functional Aspects of Extended-Spectrum AmpC Cephalosporinases, Current Drug Targets 2016; 17 (9) . https://dx.doi.org/10.2174/1573399811666150615144707

DOI https://dx.doi.org/10.2174/1573399811666150615144707	Print ISSN 1389-4501
Publisher Name Bentham Science Publisher	Online ISSN 1873-5592