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Bioorg Med Chem Lett. 2011 Dec 1;21(23):7068-71. doi: 10.1016/j.bmcl.2011.09.096. Epub 2011 Sep 29.

A small molecule that preferentially binds the closed conformation of Hsp90.

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  • 1Department of Chemistry and Biochemistry, San Diego State University, San Diego, CA 92182, USA.


Described is the synthesis of three different fluorescein-tagged derivatives of a macrocycle, and their binding affinity to heat shock protein 90 (Hsp90). Using fluorescence polarization anisotropy, we report the binding affinity of these fluorescein-labeled compounds to Hsp90 in its open state and ATP-dependent closed state. We show that the compounds demonstrate a conformation-dependent preference for binding to the closed state.

Published by Elsevier Ltd.

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