1. Hematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograft model.
- Author
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Hung MS, Xu Z, Chen Y, Smith E, Mao JH, Hsieh D, Lin YC, Yang CT, Jablons DM, and You L
- Subjects
- Animals, Blotting, Western, Casein Kinase II metabolism, Female, Hematoxylin pharmacology, Humans, Immunoenzyme Techniques, Lung Neoplasms metabolism, Lung Neoplasms pathology, Mice, Mice, Inbred BALB C, Phosphorylation drug effects, Proto-Oncogene Proteins c-akt metabolism, T Cell Transcription Factor 1 metabolism, Tumor Cells, Cultured, Wnt Proteins metabolism, Xenograft Model Antitumor Assays, Apoptosis drug effects, Casein Kinase II antagonists & inhibitors, Enzyme Inhibitors pharmacology, Hematoxylin analogs & derivatives, Lung Neoplasms prevention & control
- Abstract
Casein kinase II (CK2) inhibitors suppress cancer cell growth. In this study, we examined the inhibitory effects of a novel CK2 inhibitor, hematein, on tumor growth in a murine xenograft model. We found that in lung cancer cells, hematein inhibited cancer cell growth, Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increased apoptosis. In a murine xenograft model of lung cancer, hematein inhibited tumor growth without significant toxicity to the mice tested. Molecular docking showed that hematein binds to CK2α in durable binding sites. Collectively, our results suggest that hematein is an allosteric inhibitor of protein kinase CK2 and has antitumor activity to lung cancer.
- Published
- 2013
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