Fusidic Acid: A Bacterial Elongation Factor Inhibitor for the Oral Treatment of Acute and Chronic Staphylococcal Infections
Fusidic Acid: A Bacterial Elongation Factor Inhibitor for the Oral Treatment of Acute and Chronic Staphylococcal Infections
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DOI：
10.1101/cshperspect.a025437
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发表时间：
2016-01-01
影响因子：
5.4
通讯作者：
Fernandes, Prabhavathi
中科院分区：
文献类型：
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作者：
Fernandes, Prabhavathi
福西地酸是一种口服抗葡萄球菌抗生素，在欧洲已经使用了40多年，用于治疗皮肤感染以及慢性骨和关节感染。它是一种甾体抗生素，也是唯一上市的呋喃类抗生素。氟西地酸通过结合EF-G-GDP抑制蛋白质合成，从而抑制肽易位和核糖体拆卸。它具有新颖的结构和作用方式，因此与其他已知抗生素几乎没有交叉耐药。编码EF-G的FusA基因可能发生许多突变，其中一些突变可导致高水平耐药性（最低抑制浓度[MIC] bb0 64 mg/L），而其他突变则导致生物学上不适应的葡萄球菌，需要代偿性突变才能存活。低阻力(
Fusidic acid is an oral antistaphylococcal antibiotic that has been used in Europe for more than 40 years to treat skin infections as well as chronic bone and joint infections. It is a steroidal antibiotic and the only marketed member of the fusidane class. Fusidic acid inhibits protein synthesis by binding EF-G-GDP, which results in the inhibition of both peptide translocation and ribosome disassembly. It has a novel structure and novel mode of action and, therefore, there is little cross-resistance with other known antibiotics. Many mutations can occur in the FusA gene that codes for EF-G, and some of these mutations can result in high-level resistance (minimum inhibitory concentration [MIC] > 64 mg/L), whereas others result in biologically unfit staphylococci that require compensatory mutations to survive. Low-level resistance (