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Structure Guided Development of Potent Reversibly Binding Penicillin Binding Protein Inhibitors

  作者 WOON ESTHER C Y; ZERVOSEN ASTRID; SAUVAGE ERIC; SIMMONS KATIE J; ZIVEC MATEJ; INGLIS STEVEN R; FISHWICK COLIN W G; GOBEC STANISLAV; CHARLIER PAULETTE; LUXEN ANDRE; SCHOFIELD CHRISTOPHER J  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2011年2-3;  页码  219-223  
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[摘要]Following from the evaluation of different 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 beta-lactams.

 
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