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PDBsum entry 2ax0
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References listed in PDB file
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Key reference
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Title
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Sar and mode of action of novel non-Nucleoside inhibitors of hepatitis c ns5b RNA polymerase.
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Authors
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J.P.Powers,
D.E.Piper,
Y.Li,
V.Mayorga,
J.Anzola,
J.M.Chen,
J.C.Jaen,
G.Lee,
J.Liu,
M.G.Peterson,
G.R.Tonn,
Q.Ye,
N.P.Walker,
Z.Wang.
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Ref.
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J Med Chem, 2006,
49,
1034-1046.
[DOI no: ]
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PubMed id
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Abstract
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Novel non-nucleoside inhibitors of the HCV RNA polymerase (NS5b) with
sub-micromolar biochemical potency have been identified which are selective for
the inhibition of HCV NS5b over other polymerases. The structures of the
complexes formed between several of these inhibitors and HCV NS5b were
determined by X-ray crystallography, and the inhibitors were found to bind in an
allosteric binding site separate from the active site. Structure-activity
relationships and structural studies have identified the mechanism of action for
compounds in this series, several of which possess drug-like properties, as
unique, reversible, covalent inhibitors of HCV NS5b.
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