Designing an Inhibitor for AAC(6¿)-Ii
Fragment-based Drug Design using SAR by NMR
Herausgegeben: Auclair, Karine; Mittermaier, Anthony
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Aminoglycosides are valuable broad-spectrum antibiotics effective in both Gram-positive and Gram-negative bacteria. Antibiotic resistance has however been a scourge since the advent of modern antibiotics. One of the main mechanisms of resistance to aminoglycosides is antibiotic modification by the clinically widespread enzyme aminoglycoside N-6'-acetyltransferase. Inhibiting resistance-causing enzymes is an important strategy among the multiple approaches to counter antibiotic resistance. The Auclair lab has previously developed a series of aminoglycoside-coenzyme A bisubstrates that was found...
Aminoglycosides are valuable broad-spectrum antibiotics effective in both Gram-positive and Gram-negative bacteria. Antibiotic resistance has however been a scourge since the advent of modern antibiotics. One of the main mechanisms of resistance to aminoglycosides is antibiotic modification by the clinically widespread enzyme aminoglycoside N-6'-acetyltransferase. Inhibiting resistance-causing enzymes is an important strategy among the multiple approaches to counter antibiotic resistance. The Auclair lab has previously developed a series of aminoglycoside-coenzyme A bisubstrates that was found to be potent inhibitors of AAC(6')-Ii, but lacked activity in cell-based assays. In order to combat aminoglycoside resistance, this book aims at developing a new class of AAC(6') inhibitors using fragment-based drug design with NMR-based assays for the initial screening. This approach has the advantage of potentially identifying new structural scaffolds that are fundamentally different fromthose that have been previously developed in the group.
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