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A new bacterial mannosidase for the selective modification of ramoplanin and its derivatives

机译:一种用于选择性修饰雷莫拉宁及其衍生物的新型细菌甘露糖苷酶

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摘要

Ramoplanin is a lipoglycodepsipeptide produced by Actinoplanes sp. ATCC 33076 and active on bacterial cell wall biosynthesis by binding to Lipid II. A screening of an actinomycetes collection was performed to select enzymatic activities able to introduce specific modifications in the ramoplanin molecule. An extracellular mannosidase from Streptomyces GE 91081 was found to selectively remove one mannose unit from ramoplanin and tetrahydroramoplanin to give the corresponding mannosyl aglycones. These molecules show an improved microbiological activity versus some resistant staphylococci and streptococci, and are useful intermediates in the synthesis of novel ramoplanin-like antibiotics. The biotransformation of ramoplanin has been optimised to improve molar conversion and the transformation reaction rate.
机译:拉莫普林是由Actinoplanes sp。生产的脂糖肽肽。 ATCC 33076并通过与脂质II结合对细菌细胞壁生物合成具有活性。进行放线菌收集的筛选以选择能够在雷莫普林素分子中引入特定修饰的酶活性。发现来自链霉菌属GE 91081的细胞外甘露糖苷酶选择性地从雷莫拉宁和四氢ramoplanin中除去一个甘露糖单元,得到相应的甘露糖苷苷元。这些分子相对于一些抗性葡萄球菌和链球菌显示出改善的微生物活性,并且是合成新型雷莫拉宁类抗生素的有用中间体。优化了雷莫拉宁的生物转化,以提高摩尔转化率和转化反应速率。

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