Novel non-β-lactam inhibitor of β-lactamase TEM-171 based on acylated phenoxyaniline

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• 作者：V.G. Grigorenko^a ; ^{vitaly.grigorenko@gmail.com} ; I.P. Andreeva^a ; M.Yu. Rubtsova^a ; I.M. Deygen^a ; R.L. Antipin^a ; A.G. Majouga^a ; A.M. Egorov^a ; D.A. Beshnova^b ; J. Kallio^b ; C. Hackenberg^b ; V.S. Lamzin^b
• 关键词：Recombinant β-lactamase TEM ; Non-β-lactam inhibitor ; Lead discovery ; Antibiotic resistance
• 刊名：Biochimie
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：132
• 期：Complete
• 页码：45-53
• 全文大小：1494 K
• 卷排序：132

文摘

New type of non-β-lactam β-lactamase inhibitor based on phenoxyaniline is described. A new binding mode – blocking access to the active site is proposed. Binding of PA-34 inhibitor is assisted by at least two highly conserved residues. These residues (G242 and Y105) are conserved among molecular class A β-lactamases.