Published December 15, 2006
| public
Journal Article
Exploring the limits of benzimidazole DNA-binding oligomers for the hypoxia inducible factor (HIF) site
- Creators
- Viger, Anne
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Dervan, Peter B.
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.
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.Additional details
- Eprint ID
- 66754
- DOI
- 10.1016/j.bmc.2006.08.028
- Resolver ID
- CaltechAUTHORS:20160509-110450888
- GM-27681
- NIH
- Swiss National Science Foundation (SNSF)
- Created
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2016-05-17Created from EPrint's datestamp field
- Updated
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2021-11-11Created from EPrint's last_modified field