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Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors

2018; Multidisciplinary Digital Publishing Institute; Volume: 23; Issue: 2 Linguagem: Inglês

10.3390/molecules23020284

1433-1373

Sandra G. Zárate, M. De la Cruz Claure, Raúl Benito-Arenas, Julia Revuelta, Andrés G. Santana, Ágatha Bastida,

Biochemical and Structural Characterization

Resistance to aminoglycoside antibiotics has had a profound impact on clinical practice. Despite their powerful bactericidal activity, aminoglycosides were one of the first groups of antibiotics to meet the challenge of resistance. The most prevalent source of clinically relevant resistance against these therapeutics is conferred by the enzymatic modification of the antibiotic. Therefore, a deeper knowledge of the aminoglycoside-modifying enzymes and their interactions with the antibiotics and solvent is of paramount importance in order to facilitate the design of more effective and potent inhibitors and/or novel semisynthetic aminoglycosides that are not susceptible to modifying enzymes.