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Are highly morphed peptide frameworks lurking silently in microbial genomes valuable as next generation antibiotic scaffolds?
Natural Product Reports ( IF 11.9 ) Pub Date : 2017-05-17 00:00:00 , DOI: 10.1039/c7np00011a
Christopher T. Walsh 1, 2, 3, 4
Affiliation  

Antibiotics are a therapeutic class that, once deployed, select for resistant bacterial pathogens and so shorten their useful life cycles. As a consequence new versions of antibiotics are constantly needed. Among the antibiotic natural products, morphed peptide scaffolds, converting conformationally mobile, short-lived linear peptides into compact, rigidified small molecule frameworks, act on a wide range of bacterial targets. Advances in bacterial genome mining, biosynthetic gene cluster prediction and expression, and mass spectroscopic structure analysis suggests many more peptides, modified both in side chains and peptide backbones, await discovery. Such molecules may turn up new bacterial targets and be starting points for combinatorial or semisynthetic manipulations to optimize activity and pharmacology parameters.

中文翻译:

默默地潜伏在微生物基因组中的高度变形的肽构架是否可作为下一代抗生素支架有价值?

抗生素属于治疗类,一旦部署,就会选择具有抗药性的细菌病原体,从而缩短其使用寿命。结果,不断需要新版本的抗生素。在抗生素天然产物中,变形的肽支架将构象上可移动的,短寿命的线性肽转化为紧凑的,刚性的小分子框架,可作用于多种细菌靶标。细菌基因组挖掘,生物合成基因簇的预测和表达以及质谱结构分析方面的进展表明,侧链和肽主链均被修饰的更多肽正等待发现。此类分子可能会产生新的细菌靶标,成为组合或半合成操作以优化活性和药理学参数的起点。
更新日期:2017-07-06
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