IF 4.9 1区 化学 Q1 CHEMISTRY, ORGANIC
Xingkun Li, Mengru Wang, Lixin Yin, Jiawei Cao, Rui Wang, Wei Guo, Jing Lu, Zhilong Zhao, Zixin Deng, Anwei Hou, Min Xu
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引用次数: 0

摘要

糖肽类抗生素(GPAs)是治疗耐多药革兰氏阳性感染的一线药物。对 GPAs 的耐药性要求开发新的抗生素。通过对 GPA 生物合成基因簇的系统发育重新分类,重点研究了带有七肽支架的 V 型亚群,发现了新的 GPAs--缬霉素,其第 5 位拥有前所未有的 3,5- 二羟基苯丙氨酸和 F-G 联苯交联。缬氨霉素对耐甲氧西林金黄色葡萄球菌和耐万古霉素肠球菌的临床分离株具有广泛的活性,是以耐药性为导向的药物创新的有前途的先导化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Phylogeny-Informed Discovery of New Glycopeptide Antibiotics Produced by a Minimal Biosynthetic Gene Cluster

Phylogeny-Informed Discovery of New Glycopeptide Antibiotics Produced by a Minimal Biosynthetic Gene Cluster
Glycopeptide antibiotics (GPAs) are the frontline medicines to treat multidrug-resistant Gram-positive infections. Resistance to GPAs warrants the development of new antibiotics. Phylogeny reclassification of GPA biosynthetic gene clusters with a focus on the type V subgroup bearing a heptapeptide scaffold identified new GPAs, varsomycins, possessing unprecedented 3,5-dihydroxyphenylalanine at position 5 and an F-G biphenyl cross-link. Varsomycins are broadly active against clinical isolates of methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus and are promising lead compounds for resistance-oriented drug innovation.
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来源期刊
Organic Letters
Organic Letters 化学-有机化学
CiteScore
9.30
自引率
11.50%
发文量
1607
审稿时长
1.5 months
期刊介绍: Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.
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