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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Platensimycin and platencin: promising antibiotics for future application in human medicine.
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Platensimycin and platencin: promising antibiotics for future application in human medicine.

机译：Platensimycin和Platencin：有望在人类医学中应用的抗生素。

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摘要

Platensimycin and platencin are novel antibiotics produced by Streptomyces platensis. They are potent and non-toxic natural products active against Gram-positive pathogens, including antibiotic-resistant strains and Mycobacterium tuberculosis. They were isolated using an intriguing target-based whole-cell antisense differential sensitivity assay as inhibitors of fatty acid biosynthesis of type II. This type of biosynthesis is not present in humans. Platensimycin inhibits the elongation-condensing enzyme FabF, whereas platencin inhibits both FabF and FabH. For these antibiotics to become successful drugs, their pharmacokinetics must be improved. They have too high a rate of clearance in the body, yielding a low degree of systematic exposure. They work well when administered by continuous infusion, but this is not a useful method of delivery to patients. The two antibiotics and many analogs have been prepared by chemical synthesis. Natural congeners have also been obtained from the producing actinomycete. However, none of these molecules are as active as platensimycin and platencin. Using tools of rational metabolic engineering, superior strains have been produced making hundreds of times more antibiotic than the natural strains.
机译：Platensimycin和Platencin是由链霉菌产生的新型抗生素。它们是有效且无毒的天然产物，对革兰氏阳性病原体具有活性，包括抗药性菌株和结核分枝杆菌。使用引人入胜的基于靶标的全细胞反义差分敏感性测定法分离它们，作为II型脂肪酸生物合成的抑制剂。这种类型的生物合成在人类中不存在。板霉素抑制延伸缩合酶FabF，而板霉素则抑制FabF和FabH。为了使这些抗生素成为成功的药物，必须改善它们的药代动力学。它们在体内的清除率过高，导致较低的系统暴露度。当通过连续输注给药时，它们效果很好，但这不是向患者输送的有用方法。两种抗生素和许多类似物已通过化学合成制备。天然同源物也已从生产放线菌获得。但是，这些分子都没有像板霉素和板霉素那样具有活性。使用合理的代谢工程工具，已产生出比天然菌株高出数百倍的抗菌素。

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