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A Systematic Protocol for the Characterization of Hsp90 Modulators
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.
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.
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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.
Date
2010-10-19
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Elsevier
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Keywords
Heat shock protein 90, Novobiocin, Geldanamycin, Celastrol, Gedunin
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.