Journal
JOURNAL OF NATURAL PRODUCTS
Volume 70, Issue 12, Pages 2014-2018Publisher
AMER CHEMICAL SOC
DOI: 10.1021/np070190s
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Funding
- NCI NIH HHS [R01 CA114393] Funding Source: Medline
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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.
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