Derrubone, an inhibitor of the Hsp90 protein folding machinery

被引：58

作者：

Hadden, M. Kyle ^{[1
]}

Galam, Lakshmi ^{[2
]}

Gestwicki, Jason E. ^{[3
,4
]}

Matts, Robert L. ^{[2
]}

Blagg, Brian S. J. ^{[1
]}

机构：

[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA

[2] Oklahoma State Univ, Dept Biochem & Mol Biol, Stillwater, OK 74078 USA

[3] Univ Michigan, Dept Pathol, Ann Arbor, MI 48109 USA

[4] Univ Michigan, Life Sci Inst, Ann Arbor, MI 48109 USA

来源：

JOURNAL OF NATURAL PRODUCTS | 2007年 / 70卷 / 12期

关键词：

D O I：

10.1021/np070190s

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

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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页码：2014 / 2018

页数：5

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