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  • Title: Derrubone, an inhibitor of the Hsp90 protein folding machinery.
    Author: Hadden MK, Galam L, Gestwicki JE, Matts RL, Blagg BS.
    Journal: J Nat Prod; 2007 Dec; 70(12):2014-8. PubMed ID: 18020309.
    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.
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