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Activation of gene expression by small molecule transcription factors

Mapp, Anna K. and Ansari, Aseem Z. and Ptashne, Mark and Dervan, Peter B. (2000) Activation of gene expression by small molecule transcription factors. Proceedings of the National Academy of Sciences of the United States of America, 97 (8). pp. 3930-3935. ISSN 0027-8424. PMCID PMC18119.

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Eukaryotic transcriptional activators are minimally comprised of a DNA binding domain and a separable activation domain; most activator proteins also bear a dimerization module. We have replaced these protein modules with synthetic counterparts to create artificial transcription factors. One of these, at 4.2 kDa, mediates high levels of DNA site-specific transcriptional activation in vitro. This molecule contains a sequence-specific DNA binding polyamide in place of the typical DNA binding region and a nonprotein linker in place of the usual dimerization peptide. Thus our activating region, a designed peptide, functions outside of the archetypal protein context, as long as it is tethered to DNA. Because synthetic polyamides can, in principle, be designed to recognize any specific sequence, these results represent a key step toward the design of small molecules that can up-regulate any specified gene.

Item Type:Article
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URLURL TypeDescription CentralArticle
Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2000 by the National Academy of Sciences. Contributed by Peter B. Dervan, February 15, 2000. We thank X. Lu, S. Swalley, and E. Baird for helpful discussions and S. Malik for the Δ53pML plasmid. We are grateful to the National Institutes of Health for support of this work and for a postdoctoral fellowship to A.K.M. and to the Helen Hay Whitney foundation for a fellowship to A.Z.A. The publication costs of this article were defrayed in part by page charge payment. This article must therefore be hereby marked "advertisement" in accordance with 18 U.S.C. §1734 solely to indicate this fact.
Funding AgencyGrant Number
NIH Postdoctoral FellowshipUNSPECIFIED
Helen Hay Whitney FoundationUNSPECIFIED
Issue or Number:8
PubMed Central ID:PMC18119
Record Number:CaltechAUTHORS:MAPpnas00
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Official Citation:Anna K. Mapp, Aseem Z. Ansari, Mark Ptashne, and Peter B. Dervan Activation of gene expression by small molecule transcription factors PNAS 2000 97 (8) 3930-3935; doi:10.1073/pnas.97.8.3930
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:1502
Deposited By: Tony Diaz
Deposited On:26 Jan 2006
Last Modified:02 Oct 2019 22:44

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