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Inhibition of major-groove-binding proteins by pyrrole-imidazole polyamides with an Arg-Pro-Arg positive patch

Bremer, Ryan E. and Baird, Eldon E. and Dervan, Peter B. (1998) Inhibition of major-groove-binding proteins by pyrrole-imidazole polyamides with an Arg-Pro-Arg positive patch. Chemistry and Biology, 5 (3). pp. 119-133. ISSN 1074-5521. https://resolver.caltech.edu/CaltechAUTHORS:20160510-094623856

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Abstract

Gene-specific targeting of any protein-DNA complex by small molecules is a challenging goal at the interface of chemistry and biology. Polyamides containing N-methylimidazole and N-methylpyrrole amino acids are synthetic ligands that have an affinity and specificity for DNA comparable to many naturally occurring DNA-binding proteins. It has been shown that an eight-ring hairpin polyamide targeted to a specific minor-groove contact within a transcription factor binding site can inhibit protein-DNA binding and gene transcription. Polyamides and certain major-groove-binding proteins have been found to co-occupy the DNA helix, however. To expand the number of genes that can be targeted by pyrrole/imidazole polyamides, we set out to develop a class of polyamides that can selectively inhibit major-groove-binding proteins.


Item Type:Article
Related URLs:
URLURL TypeDescription
http://dx.doi.org/10.1016/S1074-5521(98)90057-6DOIArticle
http://www.sciencedirect.com/science/article/pii/S1074552198900576PublisherArticle
ORCID:
AuthorORCID
Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 1998 Elsevier Ltd. Received 28 November 1997, Revised 30 December 1997, and 15 January 1998, Accepted 16 January 1998, Available online 8 December 2003. We are grateful to the National Institutes of Health General Medical Sciences for research support, to the National Science Foundation for a predoctoral fellowship to R.E.B., and to the Howard Hughes Medical institute for a predoctoral fellowship to E.E.B.
Funders:
Funding AgencyGrant Number
NSF Predoctoral FellowshipUNSPECIFIED
NIHUNSPECIFIED
Howard Hughes Medical Institute (HHMI)UNSPECIFIED
Subject Keywords:DNA; hydrogen bond; minor groove; molecular recognition; transcription factor
Issue or Number:3
Record Number:CaltechAUTHORS:20160510-094623856
Persistent URL:https://resolver.caltech.edu/CaltechAUTHORS:20160510-094623856
Official Citation:Ryan E. Bremer, Eldon E. Baird, Peter B. Dervan, Inhibition of major-groove-binding proteins by pyrrole-imidazole polyamides with an Arg-Pro-Arg positive patch, Chemistry & Biology, Volume 5, Issue 3, March 1998, Pages 119-133, ISSN 1074-5521, http://dx.doi.org/10.1016/S1074-5521(98)90057-6. (http://www.sciencedirect.com/science/article/pii/S1074552198900576)
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:66868
Collection:CaltechAUTHORS
Deposited By: Victoria Brennan
Deposited On:18 May 2016 21:17
Last Modified:26 Nov 2019 11:15

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