CG0009, a Novel Glycogen Synthase Kinase 3 Inhibitor, Induces Cell Death through Cyclin D1 Depletion in Breast Cancer Cells

PLoS ONE

Volumn 8, Issue 4, 2013, Pages

  Kim, Hyun Mi ^a,b   Kim, Choung Soo ^a,b   Lee, Je Hwan ^a,b   Jang, Se Jin ^a,b   Hwang, Jung Jin ^b   Ro, Seonggu ^c   Choi, Jene ^a,b  

^a University of Ulsan College of Medicine   (South Korea)

^b Asan Medical Center   (South Korea)

^c CrystalGenomics Inc   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2,4 DICHLOROPHENYL) 3 (1 METHYL 3 INDOLYL)MALEIMIDE; 2 [4 [(2 (DIETHYLAMINO)ETHYL)(METHYL)AMINO]PHENYL] N (4 METHYLPYRIDIN 3 YL) 3H IMIDAZO[4,5 B]PYRIDINE 7 CARBOXAMIDE; BETA CATENIN; CG 0009; CYCLIN D1; ESTROGEN RECEPTOR ALPHA; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; GLYCOGEN SYNTHASE KINASE 3ALPHA; GLYCOGEN SYNTHASE KINASE 3BETA; KENPAULLONE; LITHIUM CHLORIDE; MESSENGER RNA; MYC PROTEIN; PROTEIN BAX; PROTEIN C JUN; PROTEIN KINASE B; PROTEIN P53; SERINE; TYROSINE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; BREAST CANCER; CANCER CELL CULTURE; CANCER INHIBITION; CELL ASSAY; CELL VIABILITY; CONTROLLED STUDY; DOWN REGULATION; DRUG CYTOTOXICITY; DRUG EFFICACY; DRUG MECHANISM; DRUG STRUCTURE; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; GENE CONTROL; GENE EXPRESSION; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; ONCOGENE C JUN; ONCOGENE C MYC; PROTEIN EXPRESSION; PROTEIN LOCALIZATION; QUANTITATIVE ANALYSIS; REAL TIME POLYMERASE CHAIN REACTION; SIGNAL TRANSDUCTION; UPREGULATION; WESTERN BLOTTING;

ANTINEOPLASTIC AGENTS; APOPTOSIS; BENZAZEPINES; BREAST NEOPLASMS; CELL LINE, TUMOR; CELL SURVIVAL; CYCLIN D1; FEMALE; GLYCOGEN SYNTHASE KINASE 3; HUMANS; INDOLES; LITHIUM CHLORIDE; MALEIMIDES; REAL-TIME POLYMERASE CHAIN REACTION;

EID: 84875646887     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0060383     Document Type: Article

References (30)

1. Woodgett JR, (1990) Molecular cloning and expression of glycogen synthase kinase-3/factor A. EMBO J. 9: 2431-2438.
2. Jope RS, Johnson GV, (2004) The glamour and gloom of glycogen synthase kinase-3. Trends Biochem Sci 29: 95-102.
3. Doble BW, Woodgett JR, (2003) GSK-3: tricks of the trade for a multi-tasking kinase. J Cell Sci 116: 1175-1186.
4. Eldar-Finkelman H, (2002) Glycogen synthase kinase 3: an emerging therapeutic target. Trends Mol Med 8: 126-132.
5. Cohen P, Goedert M, (2004) GSK3 inhibitors: development and therapeutic potential. Nat Rev Drug Discov 3: 479-487.
6. van Noort M, Meeldijk J, van der Zee R, Destree O, Clevers H, (2002) Wnt signaling controls the phosphorylation status of beta-catenin. J Biol Chem 277: 17901-17905.
7. Sears R, Nuckolls F, Haura E, Taya Y, Tamai K, et al. (2000) Multiple Ras-dependent phosphorylation pathways regulate Myc protein stability. Genes Dev 14: 2501-2514.
8. Cohen ED, Tian Y, Morrisey EE, (2008) Wnt signaling: an essential regulator of cardiovascular differentiation, morphogenesis and progenitor self-renewal. Development 135: 789-798.
9. Jope RS, Yuskaitis CJ, Beurel E, (2007) Glycogen synthase kinase-3 (GSK3): inflammation, diseases, and therapeutics. Neurochem Res 32: 577-595.
10. Wang Z, Smith KS, Murphy M, Piloto O, Somervaille TC, et al. (2008) Glycogen synthase kinase 3 in MLL leukaemia maintenance and targeted therapy. Nature 455: 1205-1209.
11. Tan J, Zhuang L, Leong HS, Iyer NG, Liu ET, et al. (2005) Pharmacologic modulation of glycogen synthase kinase-3beta promotes p53-dependent apoptosis through a direct Bax-mediated mitochondrial pathway in colorectal cancer cells. Cancer Res 65: 9012-9020.
12. Kotliarova S, Pastorino S, Kovell LC, Kotliarov Y, Song H, et al. (2008) Glycogen synthase kinase-3 inhibition induces glioma cell death through c-MYC, nuclear factor-kappaB, and glucose regulation. Cancer Res 68: 6643-6651.
13. Bilim V, Ougolkov A, Yuuki K, Naito S, Kawazoe H, et al. (2009) Glycogen synthase kinase-3: a new therapeutic target in renal cell carcinoma. Br J Cancer 101: 2005-2014.
14. Ougolkov AV, Fernandez-Zapico ME, Savoy DN, Urrutia RA, Billadeau DD, (2005) Glycogen synthase kinase-3beta participates in nuclear factor kappaB-mediated gene transcription and cell survival in pancreatic cancer cells. Cancer Res 65: 2076-2081.
15. Steinbrecher KA, Wilson W 3rd, Cogswell PC, Baldwin AS (2005) Glycogen synthase kinase 3beta functions to specify gene-specific, NF-kappaB-dependent transcription. Mol Cell Biol 25: 8444-8455.
16. Hoeflich KP, Luo J, Rubie EA, Tsao MS, Jin O, et al. (2000) Requirement for glycogen synthase kinase-3beta in cell survival and NF-kappaB activation. Nature 406: 86-90.
17. Ougolkov AV, Bone ND, Fernandez-Zapico ME, Kay NE, Billadeau DD, (2007) Inhibition of glycogen synthase kinase-3 activity leads to epigenetic silencing of nuclear factor kappaB target genes and induction of apoptosis in chronic lymphocytic leukemia B cells. Blood 110: 735-742.
18. Rae JM, Creighton CJ, Meck JM, Haddad BR, (2007) Johnson (2007) MDA-MB-435 cells are derived from M14 melanoma cells-a loss for breast cancer, but a boon for melanoma research. Breast Cancer Res Treat 104: 13-19.
19. Holmes T, O'Brien TA, Knight R, Lindeman R, Symonds G, et al. (2008) The role of glycogen synthase kinase-3beta in normal haematopoiesis, angiogenesis and leukaemia. Curr Med Chem 15: 1493-1499.
20. Vivanco I, Sawyers CL, (2002) The phosphatidylinositol 3-Kinase AKT pathway in human cancer. Nat. Rev. Cancer 2: 489-501.
21. Grisouard J, Medunjanin S, Hermani A, Shukla A, Mayer D, (2007) Glycogen synthase kinase-3 protects estrogen receptor alpha from proteasomal degradation and is required for full transcriptional activity of the receptor. Mol Endocrinol 21: 2427-2439.
22. Watcharasit P, Bijur GN, Song L, Zhu J, Chen X, et al. (2003) Glycogen synthase kinase-3beta (GSK3beta) binds to and promotes the actions of p53. J Biol Chem 278: 48872-48879.
23. Kunnimalaiyaan M, Vaccaro AM, Ndiaye MA, Chen H, (2007) Inactivation of glycogen synthase kinase-3beta, a downstream target of the raf-1 pathway, is associated with growth suppression in medullary thyroid cancer cells. Mol Cancer Ther 6: 1151-1158.
24. Rivest P, Renaud M, Sanderson JT, (2011) Proliferative and androgenic effects of indirubin derivatives in LNCaP human prostate cancer cells at sub-apoptotic concentrations. Chem Biol Interact 189: 177-185.
25. Armanious H, Deschenes J, Gelebart P, Ghosh S, Mackey J, et al. (2010) Clinical and biological significance of GSK-3β inactivation in breast cancer-an immunohistochemical study. Hum Pathol 41: 1657-1663.
26. Ding Q, He X, Xia W, Hsu JM, Chen CT, et al. (2007) Myeloid cell leukemia-1 inversely correlates with glycogen synthase kinase-3beta activity and associates with poor prognosis in human breast cancer. Cancer Res 67: 4564-4571.
27. Diehl JA, Cheng M, Roussel MF, Sherr CJ, (1998) Glycogen synthase kinase-3beta regulates cyclin D1 proteolysis and subcellular localization. Genes Dev 12: 3499-3511.
28. Johnson N, Speirs V, Curtin NJ, Hall AG, (2008) A comparative study of genome-wide SNP, CGH microarray and protein expression analysis to explore genotypic and phenotypic mechanisms of acquired antiestrogen resistance in breast cancer. Breast Cancer Res Treat 111: 55-63.
29. Kwek SS, Roy R, Zhou H, Climent J, Martinez-Climent JA, et al. (2009) Co-amplified genes at 8p12 and 11q13 in breast tumors cooperate with two major pathways in oncogenesis. Oncogene 28: 1892-1903.
30. Watcharasit P, Bijur GN, Zmijewski JW, Song L, Zmijewsk A, et al. (2002) Direct, activating interaction between glycogen synthase kinase-3beta and p53 after DNA damage. Proc Natl Acad Sci U S A 99: 7951-7955.