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Inhibition of DNA Binding by NF-κB with Pyrrole-Imidazole Polyamides

Wurtz, Nicholas R. and Pomerantz, Joel L. and Baltimore, David and Dervan, Peter B. (2002) Inhibition of DNA Binding by NF-κB with Pyrrole-Imidazole Polyamides. Biochemistry, 41 (24). pp. 7604-7609. ISSN 0006-2960. doi:10.1021/bi020114i.

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Synthetic ligands that bind to predetermined DNA sequences will offer a chemical approach to gene regulation if inhibition of a broad range of transcription factors can be achieved. NF-κB is a transcription factor that regulates a multitude of genes, including those involved in immune, inflammatory, and anti-apoptotic responses. NF-κB binds as heterodimer predominantly in the major groove. We report the design of polyamides that bind in the minor groove and target overlapping portions of an NF-κB binding site (5‘-GGGACTTTCC-3‘). We find that compounds that target the 5‘-GGGACT-3‘ portion of the site can inhibit DNA binding by NF-κB while those that target the 5‘-ACTTTCC-3‘ portion do not. Addition of NF-κB to the list of protein−DNA complexes that can be disrupted by minor groove binding ligands potentially increases the utility of polyamides as regulators of gene expression.

Item Type:Article
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Baltimore, David0000-0001-8723-8190
Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2002 American Chemical Society. Received February 7, 2002; Revised Manuscript Received April 3, 2002; Publication Date (Web): May 16, 2002. This research was supported by NIH Grant GM57148. N.R.W. was supported by predoctoral fellowships from Bristol-Myers Squibb and the Ralph M. Parsons Foundation. J.L.P. was supported by a postdoctoral fellowship from the Helen Hay Whitney Foundation and is currently a Special Fellow of the Leukemia and Lymphoma Society of America.
Funding AgencyGrant Number
Bristol-Myers SquibbUNSPECIFIED
Ralph M. Parsons FoundationUNSPECIFIED
Helen Hay Whitney FoundationUNSPECIFIED
Leukemia and Lymphoma SocietyUNSPECIFIED
Issue or Number:24
Record Number:CaltechAUTHORS:20160510-082724327
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Official Citation:Inhibition of DNA Binding by NF-κB with Pyrrole-Imidazole Polyamides Nicholas R. Wurtz, Joel L. Pomerantz, David Baltimore, and Peter B. Dervan Biochemistry 2002 41 (24), 7604-7609 DOI: 10.1021/bi020114i
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:66820
Deposited By: Victoria Brennan
Deposited On:18 May 2016 18:59
Last Modified:11 Nov 2021 00:03

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