Aminoglycoside antibiotic resistance by enzymatic deactivation.

摘要: Acquired resistance to the aminoglycoside family of antibiotics has rendered this large and important compounds virtually unusable. Resistance is primarily mediated by three classes enzymes, typically residing on transposable elements in resistant bacteria. These phosphotransferases, acetyltransferases adenyltransferases, chemically modify aminoglycosides, which either interferes with drug transport or binding at site antibacterial action, 30S ribosomal subunit. The structures several members aminoglycoside-modifying enzyme are now known, it hoped that through a better understanding these both from structural mechanistic view-point, could lead development rationally-designed novel specific structure-based inhibitors. Such developments help bring back forefront modern antimicrobial chemotherapy. This review focuses details enzymes whose crystal known implications findings for devising strategies overcome broad class antibiotics.