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Activity Improvement of Antimicrobial Peptides by a Chemical Modification Approach: Toward the Creation of Novel Types of Antimicrobial Agents

机译:通过化学修饰方法提高抗菌肽的活性:新型抗菌剂的创建

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摘要

There is currently a threat posed by the rapid emergence of antibiotic-resistant pathogens due to the abuse of conventional antibiotics. To overcome such a resistance problem, it is necessary to develop peptide agents with potent antimicrobial activities and high selectivity for target bacterial strains. Conventional approaches, such as the deletion, addition, and replacement of amino acid residues in the template peptide have been employed to alter the properties of antimicrobial peptides (AMPs). In this review, we summarize a recently developed approach, chemical modification, for the improvement of various types of naturally-occurring AMPs. By applying this design strategy to these peptide sequences, new AMPs with enhanced antimicrobial activities and improved selectivity for microorganisms have been successfully generated. This potential strategy should facilitate the creation of novel class of peptide antibiotics with properties suitable for pharmaceutical application.
机译:由于滥用常规抗生素,目前对抗生素耐药性病原体的迅速出现构成威胁。为了克服这种抗药性问题,有必要开发对目标细菌菌株具有有效抗菌活性和高选择性的肽试剂。已经采用常规方法,例如模板肽中氨基酸残基的缺失,添加和替换来改变抗微生物肽(AMP)的性质。在这篇综述中,我们总结了一种最近开发的方法,即化学修饰,用于改善各种类型的天然AMP。通过将这种设计策略应用于这些肽序列,已经成功产生了具有增强的抗菌活性和提高的对微生物选择性的新型AMP。这种潜在的策略应有助于创建具有适用于药物应用特性的新型肽类抗生素。

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