Dimeric bisbenzimidazoles inhibit the DNA methylation catalyzed by the murine Dnmt3a catalytic domain

When located in the DNA minor groove, dimeric bisbenzimidazoles DB(n) effectively inhibited in vitro the Dnmt3a catalytic domain (IC50 5-77 μM). The lowest IC50 value was observed for compound DB(11) with an 11-unit methylene linker joining the bisbenzimidazole fragments. Increased time of incubatio...

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Published inJournal of enzyme inhibition and medicinal chemistry Vol. 26; no. 2; pp. 295 - 300
Main Authors Cherepanova, N. A., Ivanov, A. A., Maltseva, D. V., Minero, A. S., Gromyko, A. V., Streltsov, S. A., Zhuze, A. L., Gromova, E. S.
Format Journal Article
LanguageEnglish
Published England Informa Healthcare 01.04.2011
Taylor & Francis
Subjects
Animals
Bisbenzimidazole - chemical synthesis
Bisbenzimidazole - chemistry
Bisbenzimidazole - pharmacology
Catalytic Domain
DNA Methylation - drug effects
DNA methyltransferase
DNA Modification Methylases - chemistry
DNA Modification Methylases - metabolism
Hoechst 33258
inhibition
Magnetic Resonance Spectroscopy
Mice
Molecular Structure
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Summary:When located in the DNA minor groove, dimeric bisbenzimidazoles DB(n) effectively inhibited in vitro the Dnmt3a catalytic domain (IC50 5-77 μM). The lowest IC50 value was observed for compound DB(11) with an 11-unit methylene linker joining the bisbenzimidazole fragments. Increased time of incubation of DNA with DB(n) as well as the presence of AT-clusters in DNA enhances the inhibitory effect.
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ISSN:1475-6366
1475-6374
DOI:10.3109/14756366.2010.499098