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Structure Guided Development of Potent Reversibly Binding Penicillin Binding Protein Inhibitors

机译:结构指导的有效可逆结合青霉素结合蛋白抑制剂的开发

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摘要

Following from the evaluation of diferent types of electrophiles, combined modeling and crystallographic analyses are used to generate potent boronic acid based inhibitors of a penicillin binding protein. The results suggest that a structurally informed approach to penicillin binding protein inhibition will be useful for the development of both improved reversibly binding inhibitors, including boronic acids, and acylating inhibitors, such as β-lactams.
机译:在评估了不同类型的亲电试剂之后,结合了建模和晶体学分析,以生成基于青霉素结合蛋白的强效硼酸抑制剂。结果表明,青霉素结合蛋白抑制的结构合理的方法将对开发改进的可逆结合抑制剂(包括硼酸)和酰化抑制剂(例如β-内酰胺)均有用。

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