Small Molecule Transcription Factor Mimic

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• 作者：Youngjoo Kwon ; Hans-Dieter Arndt ; Qian Mao ; Yongmun Choi ; Yoshinori Kawazoe ; Peter B. Dervan ; and Motonari Uesugi
• 刊名：Journal of the American Chemical Society
• 出版年：2004
• 出版时间：December 15, 2004
• 年：2004
• 卷：126
• 期：49
• 页码：15940 - 15941
• 全文大小：95K
• 年卷期：v.126,no.49(December 15, 2004)
• ISSN：1520-5126

文摘

Regulation of gene expression by transcription factors touches many aspects of eukaryotic biology, and its systematic, external control by organic molecules represents a challenge in chemistry. Here we report the design of a completely organic, nonpeptidic compound that mimics a transcription factor. The design takes advantage of the specific DNA-binding affinity of a hairpin polyamide molecule and the ability of wrenchnolol to bind to the Sur-2 subunit of human mediator complex. The hybrid compound of these two molecules activates transcription of a reporter gene in vitro in a promoter-dependent manner through simultaneous contacts with DNA and Sur-2. Our results indicate that it is possible to generate a transcription factor out of nonpeptidic components.