Topic
Derrubone
About: Derrubone is a research topic. Over the lifetime, 2 publications have been published within this topic receiving 78 citations.
Papers
TL;DR: High-throughput screening of a library of diverse molecules has identified derrubone, an isoflavone natural product from Derris robusta, as a potent Hsp90 inhibitor, and subsequently testing in several cellular-based assays established 1 as a low micromolar inhibitor in vitro.
Abstract: 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.
64 citations
TL;DR: These studies confirmed that the functionality present at the 3-position of the isoflavone plays a critical role in determining Hsp90 inhibition and suggests that the bicyclic ring system present in both novobiocin and derrubone do not share similar modes of binding.
37 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2010 | 1 |
| 2007 | 1 |