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Updated: Jun 14, 2026

Studies of Chaperone-Cochaperone Interactions using Homogenous Bead-Based Assay
Published on: July 21, 2021
Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity
Rongmin Zhao1, Elisa Leung, Stefan Grüner
1Department of Biochemistry, University of Toronto, Toronto, Ontario, Canada.
Background:
Hsp90 is an essential molecular chaperone that is also a novel anti-cancer drug target. There is growing interest in developing new drugs that modulate Hsp90 activity.
Methodology/Principal Findings:
Using a virtual screening approach, 4-hydroxytamoxifen, the active metabolite of the anti-estrogen drug tamoxifen, was identified as a putative Hsp90 ligand. Surprisingly, while all drugs targeting Hsp90 inhibit the chaperone ATPase activity, it was found experimentally that 4-hydroxytamoxifen and tamoxifen enhance rather than inhibit Hsp90 ATPase.
Conclusions/Significance:
Hence, tamoxifen and its metabolite are the first members of a new pharmacological class of Hsp90 activators.
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