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...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2011-04, Vol.26 (2), p.295-300
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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.
ISSN:	1475-6366 1475-6374
DOI:	10.3109/14756366.2010.499098