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 IC50 of 30 nM, but no inhibitory activity of hexahydrocurcumin up to 100 μM. In addition, curcumin can induce global DNA hypomethylation in a leukemia cell line.
Bibliographical noteFunding Information:
This work was partially supported by Grants NIH-NCI RO1 CA102031 (G.M.) and by BioMedical Mass Spectrometry Laboratory, College of Pharmacy.
- DNA hypomethylation agent