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首页> 外文期刊>Current drug metabolism >Phage Display Technique: A Novel Medicinal Approach to Overcome An tibiotic Resistance by Using Peptide-Based Inhibitors Against beta-Lactamases
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Phage Display Technique: A Novel Medicinal Approach to Overcome An tibiotic Resistance by Using Peptide-Based Inhibitors Against beta-Lactamases

机译：噬菌体展示技术：一种新的药用方法，通过使用基于肽的抑制剂对β-内酰胺酶来克服革癌的抗性

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摘要

The emergence of antibiotic resistance in bacteria is a serious threat with enormous social and economic implications. The distribution of resistance genes/markers through horizontal gene transfer leads to the dissemination of resistant strains in different parts of the world. The resistant bacteria acquire the ability to overcome resistance by different modes amongst which the expression of beta-lactamases is a major factor. The beta-lactamase enzymes cleave the amide bond of the beta-lactam antibiotics, which constitute about one-third of the antibiotics used all over the world. In a quest to control the spread of resistant bacteria, advanced generations of antibiotics are used either alone or in combination with inhibitors. However, these antibiotics and inhibitors also contain beta-lactam ring in their structure and hence are prone to be hydrolyzed by beta-lactamase enzymes in the near future. Thus, the severity of the problem is manifested due to the paucity of novel non-beta-lactam core containing antibiotics in the drug development stage. One approach to overcome these shortcomings is to use peptide-based inhibitors. Here, we describe the potential use of phage display technique to screen commercially available libraries to pan against beta-lactamase enzymes. The main advantage of using peptide-based inhibitors is that the bacteria will not be able to recruit pre-existing defense mechanisms and it will take a long time to evolve a new mechanism in its defense against peptide-based inhibitors.
机译：细菌中抗生素抗性的出现是具有巨大社会和经济影响的严重威胁。通过水平基因转移的抗性基因/标记的分布导致世界不同地区的抗性菌株的传播。抗性细菌获得了克服β-内酰胺酶表达是一种主要因素的不同模式的抗性能力。 β-内酰胺酶酶切割β-内酰胺抗生素的酰胺键，该抗生素构成世界各地抗生素的约三分之一。在寻求控制抗性细菌的扩散中，先进的抗生素单独使用或与抑制剂组合使用。然而，这些抗生素和抑制剂在其结构中也含有β-内酰胺环，因此在不久的将来，易患β-内酰胺酶的水解水解。因此，由于含有药物发育阶段的抗生素的新型非β-内酰胺核的缺乏，问题的严重程度表现出。一种克服这些缺点的方法是使用基于肽的抑制剂。这里，我们描述了噬菌体显示技术的潜在用途，以将商业上可用的文库筛选以对抗β-内酰胺酶。使用基于肽的抑制剂的主要优点是细菌不能能够招募预先存在的防御机制，并且需要很长时间才能在防御基于肽的抑制剂中发展新机制。

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