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PDBsum entry 5n8c
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References listed in PDB file
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Key reference
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Title
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Structure-Based discovery of lpxc inhibitors.
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Authors
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J.Zhang,
A.Chan,
B.Lippa,
J.B.Cross,
C.Liu,
N.Yin,
J.A.Romero,
J.Lawrence,
R.Heney,
P.Herradura,
J.Goss,
C.Clark,
C.Abel,
Y.Zhang,
K.M.Poutsiaka,
F.Epie,
M.Conrad,
A.Mahamoon,
K.Nguyen,
A.Chavan,
E.Clark,
T.C.Li,
R.K.Cheng,
M.Wood,
O.A.Andersen,
M.Brooks,
J.Kwong,
J.Barker,
I.B.Parr,
Y.Gu,
M.D.Ryan,
S.Coleman,
C.A.Metcalf.
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Ref.
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Bioorg Med Chem Lett, 2017,
27,
1670-1680.
[DOI no: ]
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PubMed id
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Abstract
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The 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.
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