Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors.

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Zarate SG, De la Cruz Claure ML, Benito-Arenas R, Revuelta J, Santana AG, Bastida A

Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors.

Molecules. 2018 Jan 30;23(2). pii: molecules23020284. doi: 10.3390/molecules23020284.

PubMed ID

29385736 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Ribostamycin	Aminoglycoside 2'-N-acetyltransferase	Protein	Mycobacterium tuberculosis	Unknown	Substrate	Details