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

Journal Article · · International Journal of Oncology
 [1];  [2];  [3];  [3];  [4];  [2];  [5];  [6];  [2];  [2]
  1. Univ. of California, San Francisco, CA (United States). Comprehensivve Cancer Center. Dept. of Surgery. Thoracic Oncology Lab.; Chang Gung Univ. of Science and Technology, Chiayi, Taiwan (Republic of China); DOE/OSTI
  2. Univ. of California, San Francisco, CA (United States). Comprehensivve Cancer Center. Dept. of Surgery. Thoracic Oncology Lab.
  3. Univ. of South Florida, Tampa, FL (United States). College of Medicine. Dept. of Molecular Medicine
  4. Lawrence Berkeley National Lab. (LBNL), Berkeley, CA (United States). Life Sciences Division
  5. Chang Gung Memorial Hospital, Taoyuan, Taiwan (Republic of China). Division of Pulmonary and Critical Care Medicine; Chang Gung Univ. of Science and Technology, Chiayi, Taiwan (Republic of China)
  6. Chang Gung Memorial Hospital, Taoyuan, Taiwan (Republic of China). Division of Pulmonary and Critical Care Medicine; Chang Gung Univ., Taoyuan, Taiwan (Republic of China). College of Medicine. Dept. of Respiratory Care
+ Show Author Affiliations
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.
Research Organization:
Lawrence Berkeley National Lab. (LBNL), Berkeley, CA (United States). National Energy Research Scientific Computing Center (NERSC)
Sponsoring Organization:
National Institutes of Health (NIH); USDOE Office of Science (SC), Biological and Environmental Research (BER). Biological Systems Science Division
Grant/Contract Number:
AC02-05CH11231
OSTI ID:
1628644
Journal Information:
International Journal of Oncology, Journal Name: International Journal of Oncology Journal Issue: 5 Vol. 43; ISSN 1019-6439
Publisher:
SpandidosCopyright Statement
Country of Publication:
United States
Language:
English

References (29)

Asymmetric Expression of Protein Kinase CK2 Subunits in Human Kidney Tumors journal July 1994
New investigations on hematoxylin, hematein, and hematein-aluminium complexes: II. Hematein-aluminium complexes and hemalum staining journal July 1991
Insights from soft X-rays: the chlorine and sulfur sub-structures of a CK2α/DRB complex journal July 2008
CK2 functionally interacts with AKT/PKB to promote the β-catenin-dependent expression of survivin and enhance cell survival journal July 2011
Too much of a good thing: The role of protein kinase CK2 in tumorigenesis and prospects for therapeutic inhibition of CK2 journal January 2008
2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole: a novel powerful and selective inhibitor of protein kinase CK2 journal September 2004
Induction of cell death in antiestrogen resistant human breast cancer cells by the protein kinase CK2 inhibitor DMAT journal October 2007
Nuclear localization of protein kinase CK2 catalytic subunit (CK2α) is associated with poor prognostic factors in human prostate cancer journal March 2007
The Raison D'Être of Constitutively Active Protein Kinases:  The Lesson of CK2 journal February 2003
Protein kinase CK2 phosphorylates and upregulates Akt/PKB journal April 2005
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA) journal September 2003
Anticomplementary Activity of Constituents from the Heartwood ofCaesalpinia sappan journal June 1998
Casein kinase 2 (CK2) increases survivin expression via enhanced beta-catenin-T cell factor/lymphoid enhancer binding factor-dependent transcription journal September 2006
One‐thousand‐and‐one substrates of protein kinase CK2? journal January 2003
Casein Kinase II in Theileriosis journal February 1995
CX-4945, an Orally Bioavailable Selective Inhibitor of Protein Kinase CK2, Inhibits Prosurvival and Angiogenic Signaling and Exhibits Antitumor Efficacy journal December 2010
Protein Kinase CK2α as an Unfavorable Prognostic Marker and Novel Therapeutic Target in Acute Myeloid Leukemia journal February 2007
Identification of hematein as a novel inhibitor of protein kinase CK2 from a natural product library journal May 2009
Hierarchical Docking of Databases of Multiple Ligand Conformations journal August 2005
Automated docking with grid-based energy evaluation journal May 1992
New investigations on hematoxylin, hematein, and hematein-aluminium complexes: II. Hematein-aluminium complexes and hemalum staining journal July 1991
Association of Elevated Protein Kinase CK2 Activity with Aggressive Behavior of Squamous Cell Carcinoma of the Head and Neck journal September 1995
The CK2α/CK2β Interface of Human Protein Kinase CK2 Harbors a Binding Pocket for Small Molecules journal February 2008
Protein kinase CK2 inhibitor 4,5,6,7-tetrabromobenzotriazole (TBB) induces apoptosis and caspase-dependent degradation of haematopoietic lineage cell-specific protein 1 (HS1) in Jurkat cells journal May 2002
Casein kinase II alpha transgene-induced murine lymphoma: relation to theileriosis in cattle journal February 1995
CX-4945, an Orally Bioavailable Selective Inhibitor of Protein Kinase CK2, Inhibits Prosurvival and Angiogenic Signaling and Exhibits Antitumor Efficacy journal December 2010
Casein Kinase II Alpha Subunit and C1-Inhibitor Are Independent Predictors of Outcome in Patients with Squamous Cell Carcinoma of the Lung journal September 2004
Protein Kinase CK2α as an Unfavorable Prognostic Marker and Novel Therapeutic Target in Acute Myeloid Leukemia journal February 2007
Antitumoral activity of allosteric inhibitors of protein kinase CK2 journal December 2011

Cited By (6)

Protein Kinase CK2, a Potential Therapeutic Target in Carcinoma Management journal January 2019
CK2 in Cancer: Cellular and Biochemical Mechanisms and Potential Therapeutic Target journal January 2017
Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7 journal January 2018
Quinalizarin, a specific CK2 inhibitor, can reduce icotinib resistance in human lung adenocarcinoma cell lines journal May 2019
Casein kinase: the triple meaning of a misnomer journal May 2014
Identification of compounds inhibiting prion replication and toxicity by removing PrP C from the cell surface journal July 2019

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