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PubMed · 15584709

Small molecule transcription factor mimic.

Youngjoo Kwon·Hans-Dieter Arndt·Qian Mao·Yongmun Choi·Yoshinori Kawazoe·Peter B Dervan·Motonari Uesugi
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Abstract

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.

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AdamantaneAvidinBiomimetic MaterialsBridged-Ring CompoundsDNA-Binding ProteinsHumansIndolesMediator ComplexNylonsPropanolsRNA Polymerase IITrans-ActivatorsTranscription FactorsJournal ArticleResearch Support, Non-U.S. Gov'tResearch Support, U.S. Gov't, Non-P.H.S.Research Support, U.S. Gov't, P.H.S.

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Youngjoo Kwon, Hans-Dieter Arndt, Qian Mao, Yongmun Choi, Yoshinori Kawazoe, Peter B Dervan, Motonari Uesugi. 2004-12-15. Small molecule transcription factor mimic.. https://doi.org/10.1021/ja0445140

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