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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2008-2-7
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pubmed:abstractText |
Heat shock protein 90 (Hsp90) is a molecular chaperone that is responsible for activating many signaling proteins and is a promising target in tumor biology. We have identified small-molecule benzisoxazole derivatives as Hsp90 inhibitors. Crystallographic studies show that these compounds bind in the ATP binding pocket interacting with the Asp93. Structure based optimization led to the identification of potent analogues, such as 13, with good biochemical profiles.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:ArndtKimK,
pubmed-author:BoschelliFrankF,
pubmed-author:ChopraRajivR,
pubmed-author:EllingboeJohnJ,
pubmed-author:GolasJenniferJ,
pubmed-author:GopalsamyAriamalaA,
pubmed-author:JacobJaisonJ,
pubmed-author:JohnsonMarkM,
pubmed-author:LeeFrederickF,
pubmed-author:MaggsF AFA,
pubmed-author:NilakantanRamaswamyR,
pubmed-author:PetersenRoseannR,
pubmed-author:ShiMengxiaoM,
pubmed-author:SvensonKristinK,
pubmed-author:VoganErikE,
pubmed-author:WenYingxiaY
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pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
373-5
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pubmed:meshHeading |
pubmed-meshheading:18197612-Adenosine Triphosphate,
pubmed-meshheading:18197612-Antineoplastic Agents,
pubmed-meshheading:18197612-Binding Sites,
pubmed-meshheading:18197612-Cell Proliferation,
pubmed-meshheading:18197612-Crystallography, X-Ray,
pubmed-meshheading:18197612-Drug Screening Assays, Antitumor,
pubmed-meshheading:18197612-HSP90 Heat-Shock Proteins,
pubmed-meshheading:18197612-Humans,
pubmed-meshheading:18197612-Isoxazoles,
pubmed-meshheading:18197612-K562 Cells,
pubmed-meshheading:18197612-Models, Molecular,
pubmed-meshheading:18197612-Protein Conformation,
pubmed-meshheading:18197612-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90.
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pubmed:affiliation |
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA. gopalsa@wyeth.com
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pubmed:publicationType |
Journal Article
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