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.
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| 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. | |||||||||
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| 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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