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PDBsum entry 4bge
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Oxidoreductase
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PDB id
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4bge
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References listed in PDB file
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Key reference
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Title
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Pyridomycin bridges the nadh- And substrate-Binding pockets of the enoyl reductase inha.
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Authors
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R.C.Hartkoorn,
F.Pojer,
J.A.Read,
H.Gingell,
J.Neres,
O.P.Horlacher,
K.H.Altmann,
S.T.Cole.
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Ref.
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Nat Chem Biol, 2014,
10,
96-98.
[DOI no: ]
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PubMed id
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Abstract
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Pyridomycin, a natural product with potent antituberculosis activity, inhibits a
major drug target, the InhA enoyl reductase. Here, we unveil the co-crystal
structure and unique ability of pyridomycin to block both the NADH cofactor- and
lipid substrate-binding pockets of InhA. This is to our knowledge a
first-of-a-kind binding mode that discloses a new means of InhA inhibition.
Proof-of-principle studies show how structure-assisted drug design can improve
the activity of new pyridomycin derivatives.
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