A small molecule that preferentially binds the closed conformation of Hsp90

作者：Alexander Leslie D; Partridge James R; Agard David A; McAlpine Shelli R^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(23): 7068-7071.

DOI：10.1016/j.bmcl.2011.09.096

• Sansalvamide A
• Hsp90
• Fluorescein
• Fluorescence polarization
• Anticancer
• Anistropy

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.

• 出版日期2011-12-1