Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.706-709
2009
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- Autor(en) / Beteiligte
- Titel
- Curcumin is a potent DNA hypomethylation agent
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.706-709
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2009
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- A potent dietary DNA methylation inhibitor, curcumin 1 (EC 50 = 30 nM) and its hypomethylation activity on MV4-11 cells (15–20% decrease in global DNA methylation) is reported. 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 μM. In addition, curcumin can induce global DNA hypomethylation in a leukemia cell line.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2008.12.041Titel-ID: cdi_proquest_miscellaneous_733631577
- Format
- –
- Schlagworte
- Antineoplastic agents, Biological and medical sciences, Catalysis, Catalytic Domain, Cell Line, Tumor, Curcumin, Curcumin - analogs & derivatives, Curcumin - chemistry, Curcumin - pharmacology, Cytosine - chemistry, DNA (Cytosine-5-)-Methyltransferase 1, DNA (Cytosine-5-)-Methyltransferases - chemistry, DNA hypomethylation agent, DNA Methylation, Dose-Response Relationship, Drug, Drug Design, General aspects, Humans, Inhibitory Concentration 50, Leukemia - drug therapy, Medical sciences, Models, Chemical, Molecular Conformation, Pharmacology. Drug treatments