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Tetracycline antibiotics and resistance mechanisms

机译:四环素类抗生素及其耐药机制

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摘要

The ribosome and protein synthesis are major targets within the cell for inhibition by antibiotics, such as the tetracyclines. The tetracycline family of antibiotics represent a large and diverse group of compounds, ranging from the naturally produced chlortetracycline, introduced into medical usage in the 1940s, to second and third generation semi-synthetic derivatives of tetracycline, such as doxycycline, minocycline and more recently the glycylcycline tigecycline. Here we describe the mode of interaction of tetracyclines with the ribosome and mechanism of action of this class of antibiotics to inhibit translation. Additionally, we provide an overview of the diverse mechanisms by which bacteria obtain resistance to tetracyclines, ranging from efflux, drug modification, target mutation and the employment of specialized ribosome protection proteins.
机译:核糖体和蛋白质合成是细胞内抗生素(例如四环素)抑制的主要靶标。四环素类抗生素代表了一大类化合物,范围从1940年代引入医疗用途的天然产生的金霉素,到四环素的第二代和第三代半合成衍生物,例如强力霉素,米诺环素,最近是甘氨酰环素tigecycline。在这里,我们描述了四环素与核糖体的相互作用模式以及此类抗生素抑制翻译的作用机理。此外,我们提供了细菌获得四环素抗性的多种机制的概述,包括外排,药物修饰,靶点突变和使用特殊的核糖体保护蛋白。

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