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PDBsum entry 2azr
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References listed in PDB file
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Key reference
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Title
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Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1b inhibitors.
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Authors
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A.F.Moretto,
S.J.Kirincich,
W.X.Xu,
M.J.Smith,
Z.K.Wan,
D.P.Wilson,
B.C.Follows,
E.Binnun,
D.Joseph-Mccarthy,
K.Foreman,
D.V.Erbe,
Y.L.Zhang,
S.K.Tam,
S.Y.Tam,
J.Lee.
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Ref.
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Bioorg Med Chem Lett, 2006,
14,
2162-2177.
[DOI no: ]
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PubMed id
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Abstract
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A novel pyridothiophene inhibitor of PTP1B was discovered by rational screening
of phosphotyrosine mimics at high micromolar concentrations. The potency of this
lead compound has been improved significantly by medicinal chemistry guided by
X-ray crystallography and molecular modeling. Excellent consistency has been
observed between structure-activity relationships and structural information
from PTP1B-inhibitor complexes.
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