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

被引：19

作者：

Hung, Ming-Szu ^{[1
,2
,3
,4
]}

Xu, Zhidong ^{[1
]}

Chen, Yu ^{[5
]}

Smith, Emmanuel ^{[5
]}

Mao, Jian-Hua ^{[6
]}

Hsieh, David ^{[1
]}

Lin, Yu-Ching ^{[2
,3
,4
]}

Yang, Cheng-Ta ^{[7
,8
]}

Jablons, David M. ^{[1
]}

You, Liang ^{[1
]}

机构：

[1] Univ Calif San Francisco, Ctr Comprehens Canc, Dept Surg, Thorac Oncol Lab, San Francisco, CA 94115 USA

[2] Chang Gung Mem Hosp, Chiayi Branch, Div Pulm & Crit Care Med, Tao Yuan, Taiwan

[3] Chang Gung Univ, Coll Med, Dept Med, Tao Yuan, Taiwan

[4] Chang Gung Univ Sci & Technol, Dept Resp Care, Chiayi, Taiwan

[5] Univ S Florida, Coll Med, Dept Mol Med, Tampa, FL USA

[6] Univ Calif Berkeley, Lawrence Berkeley Natl Lab, Life Sci Div, Berkeley, CA 94720 USA

[7] Chang Gung Mem Hosp, Div Pulm & Crit Care Med, Tao Yuan, Taiwan

[8] Chang Gung Univ, Coll Med, Dept Resp Care, Tao Yuan, Taiwan

来源：

INTERNATIONAL JOURNAL OF ONCOLOGY | 2013年 / 43卷 / 05期

关键词：

hematein; casein kinase II; Wnt; lung cancer; xenograft; SQUAMOUS-CELL CARCINOMA; CK2; EXPRESSION; TUMORIGENESIS; CK2-ALPHA; SURVIVIN; SUBUNIT; AKT/PKB;

D O I：

10.3892/ijo.2013.2087

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

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 CK2 alpha 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.

引用

页码：1517 / 1522

页数：6

共 24 条

[1] NEW INVESTIGATIONS ON HEMATOXYLIN, HEMATEIN, AND HEMATEIN-ALUMINUM COMPLEXES .2. HEMATEIN-ALUMINUM COMPLEXES AND HEMALUM STAINING
BETTINGER, C
ZIMMERMANN, HW
[J]. HISTOCHEMISTRY, 1991, 96 (03) : 215 - 228
[2] Protein kinase CK2 phosphorylates and upregulates Akt/PKB
Di Maira, G
Salvi, M
Arrigoni, G
Marin, O
Sarno, S
Brustolon, F
Pinna, LA
Ruzzene, M
[J]. CELL DEATH AND DIFFERENTIATION, 2005, 12 (06) : 668 - 677
[3] Too much of a good thing: The role of protein kinase CK2 in tumorigenesis and prospects for therapeutic inhibition of CK2
Duncan, James S.
Litchfield, David W.
[J]. BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS, 2008, 1784 (01): : 33 - 47
[4] ASSOCIATION OF ELEVATED PROTEIN-KINASE CK2 ACTIVITY WITH AGGRESSIVE-BEHAVIOR OF SQUAMOUS-CELL CARCINOMA OF THE HEAD AND NECK
GAPANY, M
FAUST, RA
TAWFIC, S
DAVIS, A
ADAMS, GL
AHMED, K
[J]. MOLECULAR MEDICINE, 1995, 1 (06) : 659 - 666
[5] Identification of hematein as a novel inhibitor of protein kinase CK2 from a natural product library
Hung, Ming-Szu
Xu, Zhidong
Lin, Yu-Ching
Mao, Jian-Hua
Yang, Cheng-Ta
Chang, Pey-Jium
Jablons, David M.
You, Liang
[J]. BMC CANCER, 2009, 9
[6] Protein kinase CK2α as an unfavorable prognostic marker and novel therapeutic target in acute myeloid leukemia
Kim, Jin Seok
Eom, Ju In
Cheong, June-Won
Choi, Ae Jin
Lee, Jin Koo
Yang, Woo Ick
Min, Yoo Hong
[J]. CLINICAL CANCER RESEARCH, 2007, 13 (03) : 1019 - 1028
[7] Protein kinase CK2: Signaling and tumorigenesis in the mammary gland
Landesman-Bollag, E
Song, DH
Romieu-Mourez, R
Sussman, DJ
Cardiff, RD
Sonenshein, GE
Seldin, DC
[J]. MOLECULAR AND CELLULAR BIOCHEMISTRY, 2001, 227 (1-2) : 153 - 165
[8] Nuclear localization of protein kinase CK2 catalytic subunit (CK2α) is associated with poor prognostic factors in human prostate cancer
Laramas, Mathieu
Pasquier, Dominique
Filhol, Odile
Ringeisen, Francois
Descotes, Jean-Luc
Cochet, Claude
[J]. EUROPEAN JOURNAL OF CANCER, 2007, 43 (05) : 928 - 934
[9] Hierarchical docking of databases of multiple ligand conformations
Lorber, DM
Shoichet, BK
[J]. CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2005, 5 (08) : 739 - 749
[10] One-thousand-and-one substrates of protein kinase CK2?
Meggio, F
Pinna, LA
[J]. FASEB JOURNAL, 2003, 17 (03) : 349 - 368

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