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UDP-3-O-(R-3-hydroxymyristoyl)-N-Acetylglucosamine Deacetylase (LpxC) Inhibitors: A New Class of Antibacterial Agents

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The rapid increase of health-threatening infections by Gram-negative pathogens along with the emergence of multidrugresistant bacterial strains demands the development of novel antibiotics directed against the previously unexploited targets. One of the promising targets in Gram-negative bacteria is the zinc-dependent metalloamidase, UDP-3-O-(R-3-hydroxymyristoyl)-Nacetylglucosamine deacetylase (LpxC). LpxC catalyzes the first committed, second overall step in the biosynthetic pathway of lipid A. Thus, research on LpxC inhibitors as antibacterial agents has become an attractive field in the development of the novel antibiotic therapy of Gram-negative bacteria. In this review, we will summarize the recent progress in the studies on the structure, catalytic mechanism and regulation of LpxC and the current development of LpxC inhibitors.

Keywords: FtsH; Gram-negative bacteria; LpxC; LpxC Inhibitors; MDR; Structure; biosynthesis; lipid A; multidrugresistant; pathogens

Document Type: Research Article


Publication date: 2012-05-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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