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PDBsum entry 2byh
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References listed in PDB file
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Key reference
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Title
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3-(5-Chloro-2,4-Dihydroxyphenyl)-Pyrazole-4-Carboxamides as inhibitors of the hsp90 molecular chaperone.
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Authors
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P.A.Brough,
X.Barril,
M.Beswick,
B.W.Dymock,
M.J.Drysdale,
L.Wright,
K.Grant,
A.Massey,
A.Surgenor,
P.Workman.
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Ref.
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Bioorg Med Chem Lett, 2005,
15,
5197-5201.
[DOI no: ]
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PubMed id
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Abstract
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Information from X-ray crystal structures of Hsp90 inhibitors bound to the human
Hsp90 molecular chaperone was used to assist in the design of
3-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as novel inhibitors of
Hsp90. Accessing an extra interaction with the protein via Phe138 gave a
significant increase in binding potency compared to similar analogues that do
not make this interaction.
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