Inhibition of RNA Polymerase by Rifampicin and Rifamycin-Like Molecules.
Inhibition of RNA Polymerase by Rifampicin and Rifamycin-Like Molecules.
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DOI：
10.1128/ecosalplus.esp-0017-2019
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发表时间：
2020-04-01
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影响因子：
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通讯作者：
Zenkin, Nikolay
中科院分区：
文献类型：
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作者：
Mosaei, Hamed;Zenkin, Nikolay
RNA聚合酶（RNA polymerase, rnap）在所有生物体内完成基因表达的第一步。然而，细菌和人类RNAP之间的序列差异使细菌RNAP成为抗生素开发的一个有希望的靶点。临床上最重要和被广泛研究的一类抗生素已知能抑制细菌RNAP是利福霉素。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。在这里，我们提供了利福霉素的发现历史，其作用机制，细菌耐药性的机制，并在其进一步发展的进展概述。
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.