Exploring the limits of benzimidazole DNA-binding oligomers for the hypoxia inducible factor (HIF) site
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-1α) b...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2006-12, Vol.14 (24), p.8539-8549 |
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| creator | Viger, Anne Dervan, Peter B. |
| description | 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-1α) 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. |
| doi_str_mv | 10.1016/j.bmc.2006.08.028 |
| format | Article |
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| ispartof | Bioorganic & medicinal chemistry, 2006-12, Vol.14 (24), p.8539-8549 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Antineoplastic agents Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Deoxyribonuclease I - metabolism DNA - metabolism DNA Footprinting General aspects Humans Hypoxia-Inducible Factor 1, alpha Subunit - metabolism Medical sciences Nylons - chemical synthesis Nylons - chemistry Nylons - pharmacology Pharmacology. Drug treatments Promoter Regions, Genetic Response Elements - drug effects Transcription, Genetic - drug effects Vascular Endothelial Growth Factor A - genetics Vascular Endothelial Growth Factor A - metabolism |
| title | Exploring the limits of benzimidazole DNA-binding oligomers for the hypoxia inducible factor (HIF) site |
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