5n8c
Crystal structure of Pseudomonas aeruginosa LpxC complexed with inhibitorCrystal structure of Pseudomonas aeruginosa LpxC complexed with inhibitor
Structural highlights
FunctionLPXC_PSEAE Involved in the biosynthesis of lipid A, a phosphorylated glycolipid that anchors the lipopolysaccharide to the outer membrane of the cell. Publication Abstract from PubMedThe emergence and spread of multidrug-resistant (MDR) Gram negative bacteria presents a serious threat for public health. Novel antimicrobials that could overcome the resistance problems are urgently needed. UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) is a cytosolic zinc-based deacetylase that catalyzes the first committed step in the biosynthesis of lipid A, which is essential for the survival of Gram-negative bacteria. Our efforts toward the discovery of novel LpxC inhibitors are presented herein. Structure-based discovery of LpxC inhibitors.,Zhang J, Chan A, Lippa B, Cross JB, Liu C, Yin N, Romero JA, Lawrence J, Heney R, Herradura P, Goss J, Clark C, Abel C, Zhang Y, Poutsiaka KM, Epie F, Conrad M, Mahamoon A, Nguyen K, Chavan A, Clark E, Li TC, Cheng RK, Wood M, Andersen OA, Brooks M, Kwong J, Barker J, Parr IB, Gu Y, Ryan MD, Coleman S, Metcalf CA 3rd Bioorg Med Chem Lett. 2017 Mar 6. pii: S0960-894X(17)30228-7. doi:, 10.1016/j.bmcl.2017.03.006. PMID:28302397[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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