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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.
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Acknowledgement
The authors thank Dr. A. Jeltsch for kind gift of the Dnmt3a-CD plasmid, Dr. B. Jack from New England Biolabs for kind gift of the M.SssI plasmid, Dr. O. Kirsanova and E. Tamyar for the procedure of DNA methylation.
Declaration of interest
The work was supported by RFBR grants 10-04-00809a, 08-04-01096a, 08-03-12148-ofi; RFBR Grant 08-04-91109/CRDF RUB1-2919-MO-07 and the Program of Presidium of RAS on Molecular and Cell Biology.