Transcriptional Up-regulation in Cells Mediated by a Small Molecule

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• 作者：Steven P. Rowe ; Ryan J. Casey ; Brian B. Brennan ; Sara J. Buhrlage ; Anna K. Mapp
• 刊名：Journal of the American Chemical Society
• 出版年：2007
• 出版时间：September 5, 2007
• 年：2007
• 卷：129
• 期：35
• 页码：10654 - 10655
• 全文大小：107K
• 年卷期：v.129,no.35(September 5, 2007)
• ISSN：1520-5126

文摘

Activator artificial transcription factors, molecules that seek out specific genes and up-regulate their transcription, are desirable as mechanistic tools and as potential therapeutic agents. One challenge has been the identification of small molecule-based activator ATFs that function in cellular systems. Here we demonstrate that an amphipathic isoxazolidine activates transcription up to 80-fold in human cells when targeted to a specific promoter. Analogous to natural transcriptional activators, the function of the isoxazolidine appears to be independent of the DNA-targeting moiety, suggesting that the molecule will be effective in a variety of contexts. This is thus a critical step toward activator ATFs constructed from small molecule components.