Synthesis of Biotinylated Episilvestrol: Highly Selective Targeting of the Translation Factors eIF4AI/II

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• 作者：Jennifer M. Chambers ; Lisa M. Lindqvist ; Andrew Webb ; David C. S. Huang ; G. Paul Savage ; Mark A. Rizzacasa
• 刊名：Organic Letters
• 出版年：2013
• 出版时间：March 15, 2013
• 年：2013
• 卷：15
• 期：6
• 页码：1406-1409
• 全文大小：300K
• 年卷期：v.15,no.6(March 15, 2013)
• ISSN：1523-7052

文摘

Silvestrol (1) and episilvestrol (2) are protein synthesis inhibitors, and the former has shown efficacy in multiple mouse models of cancer; however, the selectivity of these potent cytotoxic natural products has not been described. Herein, it is demonstrated that eukaryotic initiation factors eIF4AI/II were the only proteins detected to bind silvestrol (1) and biotinylated episilvestrol (9) by affinity purification. Our study demonstrates the remarkable selectivity of these promising chemotherapeutics.