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    A Systematic Protocol for the Characterization of Hsp90 Modulators

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    Issue Date
    2010-10-19
    Author
    Matts, Robert L.
    Brandt, Gary E. L.
    Lu, Yuanming
    Dixit, Anshuman
    Mollapour, Mehdi
    Wang, Suiquan
    Donnelly, Alison C.
    Neckers, Leonard
    Verkhivker, Gennady M.
    Blagg, Brian S. J.
    Publisher
    Elsevier
    Type
    Article
    Article Version
    Scholarly/refereed, author accepted manuscript
    Metadata
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    Abstract
    Several Hsp90 modulators have been identified including the N-terminal ligand geldanamycin (GDA), the C-terminal ligand novobiocin (NB), and the co-chaperone disruptor celastrol. Other Hsp90 modulators elicit a mechanism of action that remains unknown. For example, the natural product gedunin and the synthetic anti-spermatogenic agent H2-gamendazole, recently identified Hsp90 modulators, manifest biological activity through undefined mechanisms. Herein, we report a series of biochemical techniques used to classify such modulators into identifiable categories. Such studies provided evidence that gedunin and H2-gamendazole both modulate Hsp90 via a mechanism similar to celastrol, and unlike NB or GDA.
    Description
    This is the author's accepted manuscript. Made available by the permission of the publisher.
    URI
    http://hdl.handle.net/1808/20045
    DOI
    https://doi.org/10.1016/j.bmc.2010.10.029
    Collections
    • Medicinal Chemistry Scholarly Works [244]
    Citation
    Matts, Robert L., Gary E.l. Brandt, Yuanming Lu, Anshuman Dixit, Mehdi Mollapour, Suiquan Wang, Alison C. Donnelly, Leonard Neckers, Gennady Verkhivker, and Brian S.j. Blagg. "A Systematic Protocol for the Characterization of Hsp90 Modulators." Bioorganic & Medicinal Chemistry 19.1 (2011): 684-92. doi:10.1016/j.bmc.2010.10.029.

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    KU Libraries
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    785-864-8983

    KU Libraries
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    Lawrence, KS 66045
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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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