替米考星与其他兽用大环内酯类药物在核糖体上抑制蛋白质合成的比较。
Inhibition of protein synthesis on the ribosome by tildipirosin compared with other veterinary macrolides.
机构信息
Department of Biochemistry & Molecular Biology, University of Southern Denmark, Odense, Denmark.
出版信息
Antimicrob Agents Chemother. 2012 Nov;56(11):6033-6. doi: 10.1128/AAC.01250-12. Epub 2012 Aug 27.
Abstract
Tildipirosin is a 16-membered-ring macrolide developed to treat bacterial pathogens, including Mannheimia haemolytica and Pasteurella multocida, that cause respiratory tract infections in cattle and swine. Here we evaluated the efficacy of tildipirosin at inhibiting protein synthesis on the ribosome (50% inhibitory concentration [IC(50)], 0.23 ± 0.01 μM) and compared it with the established veterinary macrolides tylosin, tilmicosin, and tulathromycin. Mutation and methylation at key rRNA nucleotides revealed differences in the interactions of these macrolides within their common ribosomal binding site.
摘要
替米考星是一种 16 元大环内酯类抗生素，用于治疗引起牛和猪呼吸道感染的细菌病原体，包括溶血曼海姆菌和多杀巴斯德菌。在这里，我们评估了替米考星抑制核糖体蛋白合成的功效（半数抑制浓度 [IC50]，0.23 ± 0.01 μM），并将其与已建立的兽医大环内酯类抗生素泰乐菌素、替米考星和泰万菌素进行了比较。关键 rRNA 核苷酸的突变和甲基化揭示了这些大环内酯类抗生素在其共同核糖体结合位点内相互作用的差异。
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本文引用的文献
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Multiplex PCR to identify macrolide resistance determinants in Mannheimia haemolytica and Pasteurella multocida.多重 PCR 鉴定溶血曼海姆菌和多杀巴斯德菌中大环内酯类耐药决定因子。
Antimicrob Agents Chemother. 2012 Jul;56(7):3664-9. doi: 10.1128/AAC.00266-12. Epub 2012 May 7.
2
Visualizing the 16-membered ring macrolides tildipirosin and tilmicosin bound to their ribosomal site.可视化十六元环大环内酯类替米考星和替米考星与核糖体结合部位。
ACS Chem Biol. 2012 Aug 17;7(8):1351-5. doi: 10.1021/cb300105p. Epub 2012 May 14.
3
Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica.在存在erm(42)和msr(E)-mph(E)基因的情况下，牛多杀性巴氏杆菌和溶血曼氏杆菌对加米霉素和替地米星的最低抑菌浓度增加。
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