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Exploring the limits of benzimidazole DNA-binding oligomers for the hypoxia inducible factor (HIF) site

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. 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
Related URLs:
URLURL TypeDescription
http://dx.doi.org/10.1016/j.bmc.2006.08.028DOIArticle
http://www.sciencedirect.com/science/article/pii/S0968089606006924PublisherArticle
ORCID:
AuthorORCID
Dervan, Peter B.0000-0001-8852-7306
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.
Funders:
Funding AgencyGrant Number
NIHGM-27681
Swiss National Science Foundation (SNSF)UNSPECIFIED
Issue or Number:24
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:26 Nov 2019 11:15

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