title: Dimeric bisbenzimidazoles inhibit the DNA methylation catalyzed by the murine Dnmt3a catalytic domain.
abstract: 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.
authors.affiliation: Chemistry Department, Moscow State University, Moscow, Russian Federation.
authors.forename: N A
authors.initials: NA
authors.lastname: Cherepanova
authors.forename: A A
authors.initials: AA
authors.lastname: Ivanov
authors.forename: D V
authors.initials: DV
authors.lastname: Maltseva
authors.forename: A S
authors.initials: AS
authors.lastname: Minero
authors.forename: A V
authors.initials: AV
authors.lastname: Gromyko
authors.forename: S A
authors.initials: SA
authors.lastname: Streltsov
authors.forename: A L
authors.initials: AL
authors.lastname: Zhuze
authors.forename: E S
authors.initials: ES
authors.lastname: Gromova
mesh_terms: D000818:Animals; D006690:Bisbenzimidazole / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020134:Catalytic Domain; D019175:DNA Methylation / Q000187:drug effects*; D015254:DNA Modification Methylases / Q000737:chemistry* / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure
chemical_list: D015254:DNA Modification Methylases; D006690:Bisbenzimidazole