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Inhibition of major groove DNA binding bZIP proteins by positive patch polyamides

Bremer, Ryan M. and Wurtz, Nicholas R. and Szewczyk, Jason W. and Dervan, Peter B. (2001) Inhibition of major groove DNA binding bZIP proteins by positive patch polyamides. Bioorganic and Medicinal Chemistry, 9 (8). pp. 2093-103. ISSN 0968-0896. doi:10.1016/S0968-0896(01)00122-5.

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Cell permeable synthetic ligands that bind to predetermined DNA sequences offer a chemical approach to gene regulation, provided inhibition of a broad range of DNA transcription factors can be achieved. DNA minor groove binding polyamides containing aminoalkyl substituents at the N-1 of a single pyrrole residue display inhibitory effects for a bZIP protein which binds exclusively in the DNA major groove. For major groove protein inhibition, specific protein-DNA contacts along the phosphate backbone were targeted with the positively charged dimethylamino substituent on the backbone of a minor groove binding polyamide hairpin. Remarkably, these polyamides bind DNA with enhanced affinity and uncompromised specificity when compared to polyamides with the aminoalkyl moiety at the C-terminus. By adding bZIP transcription factors to the class of protein-DNA complexes that can be disrupted by minor groove binding ligands, these results may increase the functional utility of polyamides as regulators of gene expression.

Item Type:Article
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Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2001 Elsevier Science Ltd. Received 30 January 2001; accepted 4 April 2001. The authors are grateful to the National Institutes of Health for research support, the National Science Foundation for a predoctoral fellowship to R.E.B., Bristol-Myers Squibb and the Ralph M. Parson Foundation for predoctoral fellowships to R.E.B. and N.R.W., and the National Institutes of Health for a research service award to J.W.S. We thank G.M. Hathaway and the Caltech Protein/Peptide Microanalytical Laboratory for MALDI-TOF mass spectrometry.
Funding AgencyGrant Number
NIH Predoctoral FellowshipUNSPECIFIED
NSF Predoctoral FellowshipUNSPECIFIED
Bristol-Myers SquibbUNSPECIFIED
Ralph M. Parsons FoundationUNSPECIFIED
Issue or Number:8
Record Number:CaltechAUTHORS:20160510-082725831
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Official Citation:Ryan E Bremer, Nicholas R Wurtz, Jason W Szewczyk, Peter B Dervan, Inhibition of major groove DNA binding bZIP proteins by positive patch polyamides, Bioorganic & Medicinal Chemistry, Volume 9, Issue 8, August 2001, Pages 2093-2103, ISSN 0968-0896, (
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:66822
Deposited By: Victoria Brennan
Deposited On:17 May 2016 20:29
Last Modified:11 Nov 2021 00:03

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