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Small Molecule Transcription Factor Mimic

2004; American Chemical Society; Volume: 126; Issue: 49 Linguagem: Inglês

10.1021/ja0445140

1943-2984

Youngjoo Kwon, Hans‐Dieter Arndt, Qian Mao, Yongmun Choi, Yoshinori Kawazoe, Peter B. Dervan, Motonari Uesugi,

Chemical Synthesis and Analysis

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.