title: Hematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograft model.
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.
authors.affiliation: Thoracic Oncology Laboratory, Department of Surgery, Comprehensive Cancer Center, University of California, San Francisco, CA 94115, USA.
authors.forename: Ming-Szu
authors.initials: MS
authors.lastname: Hung
authors.forename: Zhidong
authors.initials: Z
authors.lastname: Xu
authors.forename: Yu
authors.initials: Y
authors.lastname: Chen
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Smith
authors.forename: Jian-Hua
authors.initials: JH
authors.lastname: Mao
authors.forename: David
authors.initials: D
authors.lastname: Hsieh
authors.forename: Yu-Ching
authors.initials: YC
authors.lastname: Lin
authors.forename: Cheng-Ta
authors.initials: CT
authors.lastname: Yang
authors.forename: David M
authors.initials: DM
authors.lastname: Jablons
authors.forename: Liang
authors.initials: L
authors.lastname: You
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005260:Female; D006416:Hematoxylin / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D007124:Immunoenzyme Techniques; D008175:Lung Neoplasms / Q000378:metabolism / Q000473:pathology / Q000517:prevention & control*; D051379:Mice; D008807:Mice, Inbred BALB C; D010766:Phosphorylation / Q000187:drug effects; D051057:Proto-Oncogene Proteins c-akt / Q000378:metabolism; D051822:T Cell Transcription Factor 1 / Q000378:metabolism; D014407:Tumor Cells, Cultured; D051153:Wnt Proteins / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays
chemical_list: D004791:Enzyme Inhibitors; D051822:T Cell Transcription Factor 1; D051153:Wnt Proteins; C007915:hematein; D047390:Casein Kinase II; D051057:Proto-Oncogene Proteins c-akt; D006416:Hematoxylin