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A Systematic Protocol for the Characterization of Hsp90 Modulators
dc.contributor.author | Matts, Robert L. | |
dc.contributor.author | Brandt, Gary E. L. | |
dc.contributor.author | Lu, Yuanming | |
dc.contributor.author | Dixit, Anshuman | |
dc.contributor.author | Mollapour, Mehdi | |
dc.contributor.author | Wang, Suiquan | |
dc.contributor.author | Donnelly, Alison C. | |
dc.contributor.author | Neckers, Leonard | |
dc.contributor.author | Verkhivker, Gennady M. | |
dc.contributor.author | Blagg, Brian S. J. | |
dc.date.accessioned | 2016-02-12T21:38:09Z | |
dc.date.available | 2016-02-12T21:38:09Z | |
dc.date.issued | 2010-10-19 | |
dc.identifier.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. | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/20045 | |
dc.description | This is the author's accepted manuscript. Made available by the permission of the publisher. | en_US |
dc.description.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. | en_US |
dc.publisher | Elsevier | en_US |
dc.subject | Heat shock protein 90 | en_US |
dc.subject | Novobiocin | en_US |
dc.subject | Geldanamycin | en_US |
dc.subject | Celastrol | en_US |
dc.subject | Gedunin | en_US |
dc.title | A Systematic Protocol for the Characterization of Hsp90 Modulators | en_US |
dc.type | Article | |
kusw.kuauthor | Blagg, Brian S. J. | |
kusw.kudepartment | Medicinal Chemistry | en_US |
dc.identifier.doi | 10.1016/j.bmc.2010.10.029 | |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | |
kusw.oapolicy | This item meets KU Open Access policy criteria. | |
dc.rights.accessrights | openAccess |