Abstract | BACKGROUND:
Casein kinase 2 (CK2) is involved in various cellular events such as proliferation, apoptosis, and the cell cycle. CK2 overexpression is associated with multiple human cancers and may therefore be a promising target for cancer therapy. To identity novel classes of inhibitors for CK2, we screened a natural product library obtained from National Cancer Institute. METHODS: The quantitative luminescent kinase assay ADP-Glo™ was used to screen CK2 inhibitors from the natural product library. The same assay was used to determine cell-free dose-dependent response of CK2 inhibitors and conduct a kinetic study. Docking was performed to predict the binding patterns of selected CK2 inhibitors. Western blot analysis was used to evaluate Akt phosphorylation specific to CK2 and apoptosis effect. The cell viability assay CellTiter-Glo(®) was used to evaluate the inhibition effects of CK2 inhibitors on cancer cells. RESULTS: CONCLUSION: Our study shows that coumestrol, a novel ATP competitive and cell permeable CK2 inhibitor with submicromolar IC(50), had inhibition effects on the growth of three cancer cell lines and may represent a promising class of CK2 inhibitors.
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Authors | Shu Liu, David Hsieh, Yi-Lin Yang, Zhidong Xu, Csaba Peto, David M Jablons, Liang You |
Journal | BMC pharmacology & toxicology
(BMC Pharmacol Toxicol)
Vol. 14
Pg. 36
(Jul 11 2013)
ISSN: 2050-6511 [Electronic] England |
PMID | 23845105
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
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Chemical References |
- Biological Products
- Protein Kinase Inhibitors
- Small Molecule Libraries
- Casein Kinase II
- Coumestrol
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Topics |
- Apoptosis
(drug effects)
- Biological Products
(pharmacology)
- Casein Kinase II
(antagonists & inhibitors)
- Cell Line, Tumor
- Cell Survival
(drug effects)
- Coumestrol
(pharmacology)
- Humans
- Molecular Docking Simulation
- National Cancer Institute (U.S.)
- Protein Kinase Inhibitors
(pharmacology)
- Small Molecule Libraries
- United States
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