| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375632 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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 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.
Graphical abstractA potent dietary DNA methylation inhibitor, curcumin 1 (EC50 = 30 nM) and its hypomethylation activity on MV4-11 cells (15–20% decrease in global DNA methylation) is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Zhongfa Liu, Zhiliang Xie, William Jones, Ryan E. Pavlovicz, Shujun Liu, Jianhua Yu, Pui-kai Li, Jiayuh Lin, Jame R. Fuchs, Guido Marcucci, Chenglong Li, Kenneth K. Chan,