Hematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograft model.

TitleHematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograft model.
Publication TypeJournal Article
Year of Publication2013
AuthorsHung M-S, Xu Z, Chen Y, Smith E, Mao J-H, Hsieh D, Lin Y-C, Yang C-T, Jablons DM, You L
JournalInt J Oncol
Volume43
Pagination1517-22
Date Published2013 Nov
ISSN1791-2423
KeywordsAnimals, Apoptosis, Blotting, Casein Kinase II, Cultured, Enzyme Inhibitors, Female, Hematoxylin, Humans, Immunoenzyme Techniques, Inbred BALB C, Lung Neoplasms, Mice, Phosphorylation, Proto-Oncogene Proteins c-akt, T Cell Transcription Factor 1, Tumor Cells, Western, Wnt Proteins, Xenograft Model Antitumor Assays
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.

DOI10.3892/ijo.2013.2087