Kinetic characterization and molecular docking of novel allosteric inhibitors of aminoglycoside phosphotransferases

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• 作者：Nadia Leban^a ; ¹ ; Elise Kaplan^a ; ² ; Laurent Chaloin^a ; Sylvain Godreuil^b ; Corinne Lionne^a ; ³ ; ^{lionne@cbs.cnrs.fr}
• 关键词：AME ; aminoglycoside-modifying enzyme ; AAC ; aminoglycoside N-acetyltransferase ; ANT ; aminoglycoside O-nucleotidyltransferase ; APH ; aminoglycoside O-phosphotransferase ; GOLD ; Genetic Optimization for Ligand Docking
• 刊名：Biochimica et Biophysica Acta (BBA) - General Subjects
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：1861
• 期：1
• 页码：3464-3473
• 全文大小：1726 K
• 卷排序：1861

文摘

We identified allosteric APH inhibitors that bind to small protein cavities The strategy is to block the enzyme function by perturbing its dynamics Basis for combined therapies development that reverse aminoglycoside resistance