Hydrating for Resistance to Radicicol

Duerfeldt, Adam S.; Blagg, Brian S. J.

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Issue Date

2009-04-17

Author

Duerfeldt, Adam S.

Blagg, Brian S. J.

Publisher

ACS Chem Biol.

Type

Article

Article Version

Scholarly/refereed, author accepted manuscript

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Abstract

Resistance to Hsp90 inhibition has become an important concern as several clinical trials are currently in progress for the treatment of cancer. A summary of known mechanisms of resistance to Hsp90 inhibitors is provided, including the recent solution of the Humicola fuscoatra Hsp90 structure, the organism responsible for the biosynthesis of radicicol. Through careful analyses of Hsp90 structures, a plausible mechanism for resistance to Hsp90 inhibitors has been obtained by single mutations about the N-terminal ATP-binding site.

Citation

Duerfeldt, A. S., & Blagg, B. S. J. (2009). Hydrating for Resistance to Radicicol. ACS Chemical Biology, 4(4), 245–247. http://doi.org/10.1021/cb9000712

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