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An Acyl-Linked Dimer of Daptomycin Is Strongly Inhibited by the Bacterial Cell Wall
ACS Infectious Diseases ( IF 5.3 ) Pub Date : 2017-03-29 00:00:00 , DOI: 10.1021/acsinfecdis.7b00019
Robert M. Taylor 1 , Bradley Scott 1 , Scott Taylor 1 , Michael Palmer 1
Affiliation  

The lipopeptide antibiotic daptomycin is active against Gram-positive pathogens. It permeabilizes bacterial cell membranes, which involves the formation of membrane-associated oligomers. We here studied a dimer of daptomycin whose two subunits were linked through a bivalent aliphatic acyl chain. Unexpectedly, the dimer had very low activity on vegetative Staphylococcus aureus and Bacillus subtilis cells. However, activity resembled that of monomeric daptomycin on liposomes and on B. subtilis L-forms. These findings underscore the importance of the bacterial cell wall in daptomycin resistance.

中文翻译:

达托霉素的酰基连接二聚体被细菌细胞壁强烈抑制。

脂肽抗生素达托霉素对革兰氏阳性病原体具有活性。它使细菌细胞膜通透,这涉及膜相关寡聚物的形成。我们在这里研究了达托霉素的二聚体,其两个亚基通过二价脂族酰基链连接。出乎意料的是,该二聚体对营养性金黄色葡萄球菌枯草芽孢杆菌细胞的活性非常低。但是,其活性类似于单体达托霉素对脂质体和枯草芽孢杆菌L-型的活性。这些发现强调了细菌细胞壁在达托霉素抗性中的重要性。
更新日期:2017-03-29
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