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.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Catalysis
-
Catalytic Domain
-
Cell Line, Tumor
-
Curcumin / analogs & derivatives
-
Curcumin / chemistry
-
Curcumin / pharmacology*
-
Cytosine / chemistry
-
DNA (Cytosine-5-)-Methyltransferase 1
-
DNA (Cytosine-5-)-Methyltransferases / chemistry
-
DNA Methylation*
-
Dose-Response Relationship, Drug
-
Drug Design
-
Humans
-
Inhibitory Concentration 50
-
Leukemia / drug therapy
-
Models, Chemical
-
Molecular Conformation
Substances
-
tetrahydrocurcumin
-
Cytosine
-
DNA (Cytosine-5-)-Methyltransferase 1
-
DNA (Cytosine-5-)-Methyltransferases
-
DNMT1 protein, human
-
Curcumin