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Review
. 2016 Jun 1;6(6):a027029.
doi: 10.1101/cshperspect.a027029.

Aminoglycosides: An Overview

Affiliations
Review

Aminoglycosides: An Overview

Kevin M Krause et al. Cold Spring Harb Perspect Med. .

Abstract

Aminoglycosides are natural or semisynthetic antibiotics derived from actinomycetes. They were among the first antibiotics to be introduced for routine clinical use and several examples have been approved for use in humans. They found widespread use as first-line agents in the early days of antimicrobial chemotherapy, but were eventually replaced in the 1980s with cephalosporins, carbapenems, and fluoroquinolones. Aminoglycosides synergize with a variety of other antibacterial classes, which, in combination with the continued increase in the rise of multidrug-resistant bacteria and the potential to improve the safety and efficacy of the class through optimized dosing regimens, has led to a renewed interest in these broad-spectrum and rapidly bactericidal antibacterials.

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Figures

Figure 1.
Figure 1.
Structures of representative aminoglycosides, including the atypical aminoglycosides streptomycin and apramycin, 4,6-substituted AGs tobramycin, gentamcin, and amikacin, and the 4,5-substituted AG neomycin. The deoxystreptamine or streptidine rings are in bold.
Figure 2.
Figure 2.
Sites of chemical modification by representative aminoglycoside-modifying enzymes (AMEs) on kanamycin A.
Figure 3.
Figure 3.
Examples of aminoglycoside modification by AMEs. (A) An example of chemical modification of gentamicin catalyzed by the aminoglycoside acetyltransferase AAC(3). (B) An example of chemical modification catalyzed by the aminoglycoside phosphotransferase APH(3′) on amikacin. (C) Adenylation of the 2″ hydroxyl of kanamycin A catalyzed by the aminoglycoside nucleotidyltransferase ANT(2″).
Figure 4.
Figure 4.
Structures of plazomicin and arbekacin.

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