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核糖体靶向抗生素及细菌耐药机制。

Ribosome-targeting antibiotics and mechanisms of bacterial resistance.

机构信息

Gene Center and Department for Biochemistry, Feodor-Lynenstr. 25, University of Munich, 81377 Munich, Germany.

出版信息

Nat Rev Microbiol. 2014 Jan;12(1):35-48. doi: 10.1038/nrmicro3155.

DOI:10.1038/nrmicro3155
PMID:24336183
Abstract

The ribosome is one of the main antibiotic targets in the bacterial cell. Crystal structures of naturally produced antibiotics and their semi-synthetic derivatives bound to ribosomal particles have provided unparalleled insight into their mechanisms of action, and they are also facilitating the design of more effective antibiotics for targeting multidrug-resistant bacteria. In this Review, I discuss the recent structural insights into the mechanism of action of ribosome-targeting antibiotics and the molecular mechanisms of bacterial resistance, in addition to the approaches that are being pursued for the production of improved drugs that inhibit bacterial protein synthesis.

摘要

核糖体是细菌细胞中主要的抗生素靶标之一。天然产生的抗生素及其半合成衍生物与核糖体颗粒结合的晶体结构为其作用机制提供了无与伦比的见解,同时也为设计针对多药耐药菌的更有效的抗生素提供了帮助。在这篇综述中,我讨论了最近关于核糖体靶向抗生素作用机制和细菌耐药性的分子机制的结构见解,以及为生产抑制细菌蛋白质合成的改良药物而采用的方法。

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ChemMedChem. 2013 Dec;8(12):1954-62. doi: 10.1002/cmdc.201300323. Epub 2013 Sep 17.
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