Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 2, Pages 672-680Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.09.064
Keywords
Rotenoid; Deguelin; Natural product; Affinity tag
Funding
- Institut Universitaire de France (IUF)
- Boehringer Ingelheim Fonds
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Deguelin, a rotenoid, has emerged as an attractive pharmacophore for chemoprevention showing in vivo activity in several xenografts. Recently, several lines of evidence have suggested its mode of action may involve inhibition of HSP90, however binding in a different mode than known pharmacophores. To further probe the target of deguelin and related rotenoids, several biotin conjugates were prepared. None of the conjugates showed significant affinity for HSP90, however two conjugates showed a strong cellular co-localization with mitochondria, consistent with binding to mitochondrial complex 1. Contrarily to rotenone, deguelin and tephrosin were not found to inhibit tubulin polymerization demonstrating a dramatic pharmacological difference between these closely related rotenoids. (C) 2011 Elsevier Ltd. All rights reserved.
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