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Bioorg Med Chem Lett ; 19(3): 706-9, 2009 Feb 01.
Article in English | MEDLINE | ID: mdl-19112019

ABSTRACT

Molecular docking of the interaction of curcumin and DNMT1 suggested that curcumin covalently blocks the catalytic thiolate of C1226 of DNMT1 to exert its inhibitory effect. This was validated by showing that curcumin inhibits the activity of M. SssI with an IC(50) of 30 nM, but no inhibitory activity of hexahydrocurcumin up to 100 microM. In addition, curcumin can induce global DNA hypomethylation in a leukemia cell line.


Subject(s)
Curcumin/pharmacology , DNA Methylation , Catalysis , Catalytic Domain , Cell Line, Tumor , Curcumin/analogs & derivatives , Curcumin/chemistry , Cytosine/chemistry , DNA (Cytosine-5-)-Methyltransferase 1 , DNA (Cytosine-5-)-Methyltransferases/chemistry , Dose-Response Relationship, Drug , Drug Design , Humans , Inhibitory Concentration 50 , Leukemia/drug therapy , Models, Chemical , Molecular Conformation
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