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Small molecule transcription factor mimic

Kwon, Youngjoo and Arndt, Hans-Dieter and Mao, Qian and Choi, Yongmun and Kawazoe, Yoshinori and Dervan, Peter B. and Uesugi, Motonari (2004) Small molecule transcription factor mimic. Journal of the American Chemical Society, 126 (49). pp. 15940-15941. ISSN 0002-7863.

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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.

Item Type:Article
Related URLs:
URLURL TypeDescription Information
Arndt, Hans-Dieter0000-0002-0792-1422
Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2004 American Chemical Society. Received September 10, 2004; Publication Date (Web): November 19, 2004. We thank H. Shimogawa and H. Kigoshi for supplying synthetic intermediates, Y. Kang for a plasmid construct, and J. H. Wilson for critical review of the manuscript. Supported by NIH Grants GM071800-01 (M.U.) and GM51747 (P.B.D.), Welch Foundation Grant Q-1490 (M.U.), and U.S. Army Grant DAMD17-02-1-0277 (Y.C.). Supported by DAAD postdoctoral fellowship (H.D.A.).
Funding AgencyGrant Number
Welch FoundationQ-1490
U.S. ArmyDAMD17-02-1-0277
Deutscher Akademischer Austauschdienst (DAAD)UNSPECIFIED
Issue or Number:49
Record Number:CaltechAUTHORS:20160509-114908919
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Official Citation:Small Molecule Transcription Factor Mimic Youngjoo Kwon, Hans-Dieter Arndt, Qian Mao, Yongmun Choi, Yoshinori Kawazoe, Peter B. Dervan, and Motonari Uesugi Journal of the American Chemical Society 2004 126 (49), 15940-15941 DOI: 10.1021/ja0445140
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:66766
Deposited By: Victoria Brennan
Deposited On:17 May 2016 22:56
Last Modified:26 Nov 2019 11:15

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