利福平和类利福平分子对 RNA 聚合酶的抑制作用

Q1 Medicine

EcoSal Plus Pub Date : 2020-04-01 DOI:10.1128/ecosalplus.ESP-0017-2019

Hamed Mosaei, Nikolay Zenkin

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引用次数: 0

摘要

RNA 聚合酶（RNAP）完成了所有生物体基因表达的第一步。然而，细菌和人类 RNAP 之间的序列差异使得细菌 RNAP 有希望成为抗生素开发的目标。目前已知能抑制细菌 RNAP 的抗生素中，对临床最重要、研究最广泛的一类是利福霉素类。例如，利福霉素是目前治疗结核病的联合疗法的重要组成部分。在此，我们将概述利福霉素的发现历史、作用机制、细菌对其产生耐药性的机制以及进一步开发的进展。

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Inhibition of RNA Polymerase by Rifampicin and Rifamycin-Like Molecules.

RNA polymerases (RNAPs) accomplish the first step of gene expression in all living organisms. However, the sequence divergence between bacterial and human RNAPs makes the bacterial RNAP a promising target for antibiotic development. The most clinically important and extensively studied class of antibiotics known to inhibit bacterial RNAP are the rifamycins. For example, rifamycins are a vital element of the current combination therapy for treatment of tuberculosis. Here, we provide an overview of the history of the discovery of rifamycins, their mechanisms of action, the mechanisms of bacterial resistance against them, and progress in their further development.

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来源期刊

EcoSal Plus Immunology and Microbiology-Microbiology

CiteScore

12.20

自引率

0.00%

发文量

期刊介绍： EcoSal Plus is the authoritative online review journal that publishes an ever-growing body of expert reviews covering virtually all aspects of E. coli, Salmonella, and other members of the family Enterobacteriaceae and their use as model microbes for biological explorations. This journal is intended primarily for the research community as a comprehensive and continuously updated archive of the entire corpus of knowledge about the enteric bacterial cell. Thoughtful reviews focus on physiology, metabolism, genetics, pathogenesis, ecology, genomics, systems biology, and history E. coli and its relatives. These provide the integrated background needed for most microbiology investigations and are essential reading for research scientists. Articles contain links to E. coli K12 genes on the EcoCyc database site and are available as downloadable PDF files. Images and tables are downloadable to PowerPoint files.