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Drug Resist Updat. 2001 Apr;4(2):106-17.

Aminoglycoside-modifying enzymes: mechanisms of catalytic processes and inhibition.

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  • 1Institute for Drug Design, Departments of Chemistry, Pharmacology and Biochemistry and Molecular Biology, Wayne State University, Detroit, Michigan, USA.


The most prevalent mechanism for resistance to aminoglycoside antibiotics is mediated through their enzymatic modification in resistant organisms. Dozens of aminoglycoside-modifying enzymes are known at the gene sequence level, but few have been characterized in the details of their mechanism. This review summarizes the state of knowledge of the best studied of these enzymes, focusing on their catalytic mechanisms and inhibition.

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