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PDBsum entry 3d0b
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References listed in PDB file
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Key reference
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Title
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Discovery of benzamide tetrahydro-4h-Carbazol-4-Ones as novel small molecule inhibitors of hsp90.
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Authors
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T.E.Barta,
J.M.Veal,
J.W.Rice,
J.M.Partridge,
R.P.Fadden,
W.Ma,
M.Jenks,
L.Geng,
G.J.Hanson,
K.H.Huang,
A.F.Barabasz,
B.E.Foley,
J.Otto,
S.E.Hall.
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Ref.
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Bioorg Med Chem Lett, 2008,
18,
3517-3521.
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PubMed id
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Abstract
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Hsp90 maintains the conformational stability of multiple proteins implicated in
oncogenesis and has emerged as a target for chemotherapy. We report here the
discovery of a novel small molecule scaffold that inhibits Hsp90. X-ray data
show that the scaffold binds competitively at the ATP site on Hsp90. Cellular
proliferation and client assays demonstrate that members of the series are able
to inhibit Hsp90 at nanomolar concentrations.
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