Viger, Anne and Dervan, Peter B. (2006) Exploring the limits of benzimidazole DNA-binding oligomers for the hypoxia inducible factor (HIF) site. Bioorganic and Medicinal Chemistry, 14 (24). pp. 8539-8549. ISSN 0968-0896. doi:10.1016/j.bmc.2006.08.028. https://resolver.caltech.edu/CaltechAUTHORS:20160509-110450888
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Abstract
The vascular endothelial growth factor (VEGF) and its receptors have been implicated as key-factors in tumor angiogenesis and are major targets in cancer therapy. New oligomers which mimic the architecture of DNA-binding polyamides have been designed to target the hypoxia inducible factor (HIF-1alpha) binding site on the promoter of VEGF gene. These oligomers incorporate an increasing number of six-five fused rings such as hydroxybenzimidazole-imidazole, benzimidazole-pyrrole, benzimidazole-chlorothiophene, and imidazopyridine-pyrrole, and bind the VEGF hypoxia response element (HRE) 5'-TACGT-3' with high affinity and selectivity.
| Item Type: | Article | |||||||||
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| Additional Information: | © 2006 Elsevier. Received 18 July 2006, Revised 19 August 2006, Accepted 22 August 2006, Available online 12 September 2006. We thank B. Boras for the synthesis of 3. We thank The National Institutes of Health for grant support (GM 27681) and the Swiss National Science Foundation for a fellowship to A.V. | |||||||||
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| Issue or Number: | 24 | |||||||||
| DOI: | 10.1016/j.bmc.2006.08.028 | |||||||||
| Record Number: | CaltechAUTHORS:20160509-110450888 | |||||||||
| Persistent URL: | https://resolver.caltech.edu/CaltechAUTHORS:20160509-110450888 | |||||||||
| Official Citation: | Anne Viger, Peter B. Dervan, Exploring the limits of benzimidazole DNA-binding oligomers for the hypoxia inducible factor (HIF) site, Bioorganic & Medicinal Chemistry, Volume 14, Issue 24, 15 December 2006, Pages 8539-8549, ISSN 0968-0896, http://dx.doi.org/10.1016/j.bmc.2006.08.028. (http://www.sciencedirect.com/science/article/pii/S0968089606006924) | |||||||||
| Usage Policy: | No commercial reproduction, distribution, display or performance rights in this work are provided. | |||||||||
| ID Code: | 66754 | |||||||||
| Collection: | CaltechAUTHORS | |||||||||
| Deposited By: | Victoria Brennan | |||||||||
| Deposited On: | 17 May 2016 21:52 | |||||||||
| Last Modified: | 11 Nov 2021 00:02 |
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