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Nucleic Acids Symposium Series 2006 50(1):29-30; doi:10.1093/nass/nrl015
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© 2006 Oxford University Press

Synthesis of synthetic small molecule transcription factors (STF)

Ayato Sato1, Yoshinori Kawazoe1, Shinji Kamisuki1 and Motonari Uesugi1,2

1 Institute for Chemical Research, Kyoto university, Gokasho, Uji, Kyoto 611-0011, Japan, 2 PRESTO, JST, 4-1-8 Honcho Kawaguchi, Saitama 332-0012, Japan

External control of gene expression by small synthetic molecules represents a challenge in chemistry. Here we discuss the synthetic aspects of small molecule transcription factor mimics including a molecule we call STF1 (1). STF1 stimulates the transcription of a reporter gene controlled by specific DNA elements and behaves just as a naturally occurring transcription factor. However, STF1 had limited cell permeability, even though the hairpin-polyamide-FITC conjugate and the wrenchnolol (2) are cell permeable as separate compounds. Systematic synthetic exploration of STF1 analogs (STFs), by optimizing the physical properties of the molecule, is expected to increase its cell permeability for biological studies.


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