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PDBsum entry 2e2b
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References listed in PDB file
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Key reference
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Title
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Structural factors contributing to the abl/lyn dual inhibitory activity of 3-Substituted benzamide derivatives.
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Authors
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T.Horio,
T.Hamasaki,
T.Inoue,
T.Wakayama,
S.Itou,
H.Naito,
T.Asaki,
H.Hayase,
T.Niwa.
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Ref.
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Bioorg Med Chem Lett, 2007,
17,
2712-2717.
[DOI no: ]
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PubMed id
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Abstract
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To investigate why 3-substituted benzamide derivatives show dual inhibition of
Abl and Lyn protein tyrosine kinases, we determined their inhibitory activities
against Abl and Lyn, carried out molecular modeling, and conducted a
structure-activity relationship study with the aid of a newly determined X-ray
structure of the Abl/Lyn dual inhibitor INNO-406 (formerly known as NS-187)
bound to human Abl. We found that this series of compounds interacted with both
kinases in very similar ways, so that they can inhibit both kinases effectively.
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