State Key Laboratory of Bioreactor Engineering, Key Laboratory for Ultrafine Materials of Ministry of Education, Research Center for Biomedical Materials of Ministry of Education, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai, 200237, China.
Angew Chem Int Ed Engl. 2020 Apr 16;59(16):6412-6419. doi: 10.1002/anie.202000505.
Peptides have important biological functions. However, their susceptibility to proteolysis limits their applications. We demonstrated here for the first time, that poly(2-oxazoline) (POX) can work as a functional mimic of peptides. POX-based glycine pseudopeptides, a host defense peptide mimic, had potent activities against methicillin-resistant S. aureus, which causes formidable infections. The POX mimic showed potent activity against persisters that are highly resistant to antibiotics. S. aureus did not develop resistance to POX owning to the reactive oxygen species related antimicrobial mechanism. POX-treated S. aureus is sensitive to common antibiotics, demonstrating no observable antimicrobial pressure or cross-resistance in using antimicrobial POX. This study highlights POX as a new type of functional mimic of peptides and opens new avenues in designing and exploring peptide mimetics for biological functions and applications.
肽具有重要的生物学功能。然而，它们对蛋白水解的敏感性限制了它们的应用。我们在这里首次证明，聚（2-恶唑啉）（POX）可以作为肽的功能模拟物。基于 POX 的甘氨酸假肽，一种宿主防御肽模拟物，对引起严重感染的耐甲氧西林金黄色葡萄球菌具有很强的活性。POX 模拟物对高度耐受抗生素的持久性细菌具有很强的活性。由于与活性氧相关的抗菌机制，金黄色葡萄球菌对 POX 没有产生耐药性。POX 处理过的金黄色葡萄球菌对常用抗生素敏感，表明在使用抗菌 POX 时没有观察到明显的抗菌压力或交叉耐药性。这项研究强调了 POX 作为肽的新型功能模拟物，并为设计和探索用于生物学功能和应用的肽模拟物开辟了新途径。
