Minor groove dimeric bisbenzimidazoles inhibit in vitro DNA binding to eukaryotic DNA topoisomerase I

The potential of six dimeric bisbenzimidazoles bound to scDNA to inhibit eukaryotic DNA topoisomerase (topo-I) was studied chemically; the tested compounds differed in linker structure and length. All the compounds inhibited topo-I, DB(7) being the most efficient; its inhibitory activity in vitro wa...

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Veröffentlicht in:	Biochemistry (Moscow) 2010-06, Vol.75 (6), p.695-701
Hauptverfasser:	Susova, O. Yu, Ivanov, A. A., Morales Ruiz, S. S., Lesovaya, E. A., Gromyko, A. V., Streltsov, S. A., Zhuze, A. L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding sites Biochemistry Biomedical and Life Sciences Biomedicine Bioorganic Chemistry Bisbenzimidazole - chemistry Bisbenzimidazole - pharmacology Chemical compounds Chemical properties Deoxyribonucleic acid Dimerization DNA DNA - metabolism DNA topoisomerase I DNA Topoisomerases, Type I - metabolism DNA-ligand interactions Enzymes Genetic transcription Inhibitor drugs Life Sciences Microbiology Protein Binding Topoisomerase I Inhibitors
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Zusammenfassung:	The potential of six dimeric bisbenzimidazoles bound to scDNA to inhibit eukaryotic DNA topoisomerase (topo-I) was studied chemically; the tested compounds differed in linker structure and length. All the compounds inhibited topo-I, DB(7) being the most efficient; its inhibitory activity in vitro was 50-fold higher than that of camptothecin. It is noteworthy that inhibitory properties of nearly all the tested compounds increased many times if they were preincubated with scDNA for three days.
ISSN:	0006-2979 1608-3040
DOI:	10.1134/S0006297910060039