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Bioorg Med Chem. 2011 Jan 1;19(1):684-92. doi: 10.1016/j.bmc.2010.10.029. Epub 2010 Oct 19.

A systematic protocol for the characterization of Hsp90 modulators.

Author information

1
Department of Biochemistry and Molecular Biology, Oklahoma State University, Stillwater, OK 74078, United States.

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.

PMID:
21129982
PMCID:
PMC4618652
DOI:
10.1016/j.bmc.2010.10.029
[Indexed for MEDLINE]
Free PMC Article

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