Two Distinct Mechanisms of Inhibition of LpxA Acyltransferase Essential for Lipopolysaccharide Biosynthesis

The lipopolysaccharide biosynthesis pathway is considered an attractive drug target against the rising threat of multi-drug-resistant Gram-negative bacteria. Here, we report two novel small-molecule inhibitors (compounds 1 and 2) of the acyltransferase LpxA, the first enzyme in the lipopolysaccharid...

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Veröffentlicht in:	Journal of the American Chemical Society 2020-03, Vol.142 (9), p.4445-4455
Hauptverfasser:	Han, Wooseok, Ma, Xiaolei, Balibar, Carl J, Baxter Rath, Christopher M, Benton, Bret, Bermingham, Alun, Casey, Fergal, Chie-Leon, Barbara, Cho, Min-Kyu, Frank, Andreas O, Frommlet, Alexandra, Ho, Chi-Min, Lee, Patrick S, Li, Min, Lingel, Andreas, Ma, Sylvia, Merritt, Hanne, Ornelas, Elizabeth, De Pascale, Gianfranco, Prathapam, Ramadevi, Prosen, Katherine R, Rasper, Dita, Ruzin, Alexey, Sawyer, William S, Shaul, Jacob, Shen, Xiaoyu, Shia, Steven, Steffek, Micah, Subramanian, Sharadha, Vo, Jason, Wang, Feng, Wartchow, Charles, Uehara, Tsuyoshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Acyltransferases - antagonists & inhibitors Acyltransferases - metabolism Anti-Bacterial Agents - metabolism Anti-Bacterial Agents - pharmacology Crystallography, X-Ray Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Escherichia coli - drug effects Escherichia coli - enzymology Imidazoles - metabolism Imidazoles - pharmacology Microbial Sensitivity Tests Protein Binding Pyrazoles - metabolism Pyrazoles - pharmacology
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