MECHANISM OF ACTION OF FOSFOMYCIN (PHOSPHONOMYCIN)
MECHANISM OF ACTION OF FOSFOMYCIN (PHOSPHONOMYCIN)
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DOI：
10.1111/j.1749-6632.1974.tb43277.x
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发表时间：
1974-01-01
影响因子：
5.2
通讯作者：
KROPP, H
中科院分区：
文献类型：
--
作者：
KAHAN, FM;KAHAN, JS;KROPP, H
磷霉素是一种由链霉菌产生的新抗生素，它的发现是Hendlin及其同事在1969年以其原名磷霉素宣布的。图1所示的化学结构结合了两个不寻常的特征：一个环氧环，在抗生素中很少见;一个碳-磷键，在细菌的天然产物中首次出现。我们详细比较了该酶的催化中心对抗生素和其正常底物的作用。我们还描述了两个立体特异性营养转运系统的作用，通过介导磷霉素的进入和积累，包括各种细菌对这种极性抗生素的敏感性的决定因素。
The discovery of fosfomycin, a new antibiotic produced by strains of Streptomyces, was announced under its former name phosphonomycin by Hendlin and colleagues in 1969. l The chemical structure shown in FIGURE 1 combines two unusual features: an epoxide ring, rare among antibiotics, and a carbon-phosphorus bond which is seen to occur here for the first time among the natural products of the bacteria.Most of the present account concerns the determination of the enzymatic step in cell wall biosynthesis that is ultimately blocked by fosfomycin. We compare in detail the action of that enzyme’s catalytic center upon the antibiotic and its normal substrate. We also describe the role of two stereospecific nutrient transport systems that by mediating the entry and accumulation of fosfomycin comprise the determining factors in the sensitivity of various bacteria to this polar antibiotic.