Derrubone, an Inhibitor of the Hsp90 Protein Folding Machinery
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- 作者：M. Kyle Hadden ; Lakshmi Galam ; Jason E. Gestwicki ; Robert L. Matts ; Brian S. J. Blagg
- 刊名：Journal of Natural Products
- 出版年：2007
- 出版时间：December 2007
- 年：2007
- 卷：70
- 期：12
- 页码：2014 - 2018
- 全文大小：365K
- 年卷期：v.70,no.12(December 2007)
- ISSN：1520-6025
文摘
High-throughput screening of a library of diverse molecules has identified derrubone (1), an isoflavone natural product from Derris robusta, as a potent Hsp90 inhibitor. Subsequent testing in several cellular-based assays established 1 as a low micromolar inhibitor in vitro. In addition, derrubone induced the degradation of numerous Hsp90 client proteins, a hallmark effect resulting from Hsp90 inhibition. The identification of 1 as an Hsp90 inhibitor provides a new natural product scaffold upon which the development of novel Hsp90 inhibitors can be pursued.