The AMPK inhibitor compound C is a potent AMPK-independent antiglioma agent

Molecular Cancer Therapeutics

Volumn 13, Issue 3, 2014, Pages 596-605

  Liu, Xiaona ^a   Chhipa, Rishi Raj ^a   Nakano, Ichiro ^b   Dasgupta, Biplab ^a  

^a CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER   (United States)

^b OHIO STATE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 AMINO 4 IMIDAZOLECARBOXAMIDE RIBOSIDE; ANTINEOPLASTIC AGENT; CALPAIN; CALPAIN 1; CALPAIN 2; CATHEPSIN; CATHEPSIN B; CATHEPSIN L; DORSOMORPHIN; GLYCOGEN SYNTHASE KINASE 3BETA; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE KINASE; INITIATION FACTOR 4E; INITIATION FACTOR 4E BINDING PROTEIN 1; MAMMALIAN TARGET OF RAPAMYCIN COMPLEX 1; MAMMALIAN TARGET OF RAPAMYCIN COMPLEX 2; METFORMIN; PROTEIN KINASE B; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; ASTROCYTE; AUTOPHAGY; CANCER GROWTH; CELL COUNT; CELL MIGRATION ASSAY; CELL PROLIFERATION; CELL SURVIVAL; CONTROLLED STUDY; DRUG MECHANISM; ENZYME ACTIVATION; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; ENZYME SUBSTRATE; GLIOBLASTOMA; GLIOMA; GLIOMA CELL; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; NECROPTOSIS; PRIORITY JOURNAL; SIGNAL TRANSDUCTION;

AMP-ACTIVATED PROTEIN KINASES; APOPTOSIS; BRAIN NEOPLASMS; CELL LINE, TUMOR; CELL PROLIFERATION; GLIOMA; HUMANS; PROTEIN KINASE INHIBITORS; PYRAZOLES; PYRIMIDINES; TOR SERINE-THREONINE KINASES;

EID: 84896300923     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-13-0579     Document Type: Article

References (40)

1. Shaw RJ, Kosmatka M, Bardeesy N, Hurley RL, Witters LA, DePinho RA, et al. The tumor suppressor LKB1 kinase directly activates AMP-activated kinase and regulates apoptosis in response to energy stress. Proc Natl Acad Sci U S A 2004;101:3329-35. (Pubitemid 38338195)
2. Jones RG, Thompson CB. Tumor suppressors and cell metabolism: a recipe for cancer growth. Genes Dev 2009;23:537-48.
3. Hardie DG. AMP-activated protein kinase - an energy sensor that regulates all aspects of cell function. Genes Dev 2011;25:1895-908.
4. Viollet B, Horman S, Leclerc J, Lantier L, Foretz M, Billaud M, et al. AMPK inhibition in health and disease. Crit Rev Biochem Mol Biol 2010;45:276-95.
5. Hawley SA, Pan DA, Mustard KJ, Ross L, Bain J, Edelman AM, et al. Calmodulin-dependent protein kinase kinase-β is an alternative upstream kinase for AMP-activated protein kinase. Cell Metab 2005;2:9-19. (Pubitemid 43239821)
6. Woods A, Dickerson K, Heath R, Hong S-P, Momcilovic M, Johnstone SR, et al. Ca/calmodulin-dependent protein kinase kinase-β acts upstream of AMP-activated protein kinase in mammalian cells. Cell Metab 2005;2:21-33. (Pubitemid 43239822)
7. Foretz M, Carling D, Guichard C, Ferré P, Foufelle F. AMP-activated protein kinase inhibits the glucose-activated expression of fatty acid synthase gene in rat hepatocytes. J Biol Chem 1998;273:14767-71. (Pubitemid 28272762)
8. Guo D, Hildebrandt IJ, Prins RM, Soto H, Mazzotta MM, Dang J, et al. The AMPK agonist AICAR inhibits the growth of EGFRvIII-expressing glioblastomas by inhibiting lipogenesis. Proc Natl Acad Sci U S A 2009;106:12932-7.
9. Swinnen JV, Beckers A, Brusselmans K, Organe S, Segers J, Timmermans L, et al. Mimicry of a cellular low energy status blocks tumor cell anabolism and suppresses the malignant phenotype. Cancer Res 2005;65:2441-8. (Pubitemid 40490156)
10. Inoki K, Zhu T, Guan K-L. TSC2 mediates cellular energy response to control cell growth and survival. Cell 2003;115:577-90. (Pubitemid 37506046)
11. Gwinn DM, Shackelford DB, Egan DF, Mihaylova MM, Mery A, Vasquez DS, et al. AMPK phosphorylation of raptor mediates a metabolic checkpoint. Mol Cell 2008;30:214-26. (Pubitemid 351626684)
12. Isakovic A, Harhaji L, Stevanovic D, Markovic Z, Sumarac-Dumanovic M, Starcevic V, et al. Dual antiglioma action of metformin: cell cycle arrest and mitochondria-dependent apoptosis. Cell Mol Life Sci 2007;64:1290-302. (Pubitemid 46791062)
13. Tang YC, Williams BR, Siegel JJ, Amon A. Identification of aneuploidy-selective antiproliferation compounds. Cell 2011;144:499-512.
14. Boergermann J, Kopf J, Yu P, Knaus P. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J Biochem Cell Biol 2010;42:1802-7.
15. Paul BY, Hong CC, Sachidanandan C, Babitt JL, Deng DY, Hoyng SA, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol 2008;4:33-41. (Pubitemid 350273653)
16. Bain J, Plater L, Elliott M, Shpiro N, Hastie C, Mclauchlan H, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J 2007;408:297-315.
17. Vogt J, Traynor R, Sapkota GP. The specificities of small molecule inhibitors of the TGFss and BMP pathways. Cell Signal 2011;23:1831- 42.
18. Ríos M, Foretz M, Viollet B, Prieto A, Fraga M, Costoya JA, et al. AMPK activation by oncogenesis is required to maintain cancer cell proliferation in astrocytic tumors. Cancer Res 2013;73:2628-38.
19. Sabatini DM. mTOR and cancer: insights into a complex relationship. Nat Rev Cancer 2006;6:729-34. (Pubitemid 44286004)
20. Wullschleger S, Loewith R, Hall MN. TOR signaling in growth and metabolism. Cell 2006;124:471-84. (Pubitemid 43199434)
21. Um SH, D'Alessio D, Thomas G. Nutrient overload, insulin resistance, and ribosomal protein S6 kinase 1, S6K1. Cell Metab 2006;3:393-402. (Pubitemid 43811780)
22. Livingstone M, Atas E, Meller A, Sonenberg N. Mechanisms governing the control of mRNA translation. Phys Biol 2010;7:021001.
23. Jin J, Mullen TD, Hou Q, Bielawski J, Bielawska A, Zhang X, et al. AMPK inhibitor Compound C stimulates ceramide production and promotes Bax redistribution and apoptosis in MCF7 breast carcinoma cells. J Lipid Res 2009;50:2389-97.
24. Vucicevic L, Misirkic M, Janjetovic K, Harhaji-Trajkovic L, Prica M, Stevanovic D, et al. AMP-activated protein kinase-dependent and- independent mechanisms underlying in vitro antiglioma action of compound C. Biochem Pharmacol 2009;77:1684-93.
25. Fan QW, Cheng C, Hackett C, Feldman M, Houseman BT, Nicolaides T, et al. Akt and autophagy cooperate to promote survival of drugresistant glioma. Sci Signal 2010;3:ra81.
26. Guo JY, Chen HY, Mathew R, Fan J, Strohecker AM, Karsli-Uzunbas G, et al. Activated Ras requires autophagy to maintain oxidative metabolism and tumorigenesis. Genes Dev 2011;25:460-70.
27. Nakano A, Kato H, Watanabe T, Min KD, Yamazaki S, Asano Y, et al. AMPK controls the speed of microtubule polymerization and directional cell migration through CLIP-170 phosphorylation. Nat Cell Biol 2010;12:583-90.
28. Moser TS, Jones RG, Thompson CB, Coyne CB, Cherry S. A kinome RNAi screen identified AMPK as promoting poxvirus entry through the control of actin dynamics. PLoS Pathog 2010;6:e1000954.
29. Frigo DE, Howe MK, Wittmann BM, Brunner AM, Cushman I, Wang Q, et al. CaM kinase kinase β-mediated activation of the growth regulatory kinase AMPK is required for androgen-dependent migration of prostate cancer cells. Cancer Res 2011;71:528-37.
30. Banko MR, Allen JJ, Schaffer BE, Wilker EW, Tsou P, White JL, et al. Chemical genetic screen for AMPK α2 substrates uncovers a network of proteins involved in mitosis. Mol Cell 2011;44:878-92.
31. Dasgupta B, Milbrandt J. AMP-activated protein kinase phosphorylates retinoblastoma protein to control mammalian brain development. Dev Cell 2009;16:256-70.
32. Daub H, Olsen JV, Bairlein M, Gnad F, Oppermann FS, Körner R, et al. Kinase-selective enrichment enables quantitative phosphoproteomics of the kinome across the cell cycle. Mol Cell 2008;31:438-48.
33. Lee JH, Koh H, Kim M, Kim Y, Lee SY, Karess RE, et al. Energy-dependent regulation of cell structure by AMP-activated protein kinase. Nature 2007;447:1017-20. (Pubitemid 46975745)
34. Moffat J, Grueneberg DA, Yang X, Kim SY, Kloepfer AM, Hinkle G, et al. A lentiviral RNAi library for human and mouse genes applied to an arrayed viral high-content screen. Cell 2006;124:1283-98.
35. Bettencourt-Dias M, Giet R, Sinka R, Mazumdar A, Lock W, Balloux F, et al. Genome-wide survey of protein kinases required for cell cycle progression. Nature 2004;432:980-7. (Pubitemid 40052222)
36. Vucicevic L, Misirkic M, Kristina J, Vilimanovich U, Sudar E, Isenovic E, et al. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy 2011;7:40-50.
37. Yang WL, Perillo W, Liou D, Marambaud P, Wang P. AMPK inhibitor compound C suppresses cell proliferation by induction of apoptosis and autophagy in human colorectal cancer cells. J Surg Oncol 2012;106:680-8.
38. 2 checkpoint pathway potentiates temozolomide-induced toxicity in a p53-independent manner in human glioblastoma cells. Cancer Res 2001;61:5843-9.
39. Darzynkiewicz Z, Juan G, Li X, Gorczyca W, Murakami T, Traganos F. Cytometry in cell necrobiology: analysis of apoptosis and accidental cell death (necrosis). Cytometry 1997;27:1-20. (Pubitemid 27059777)
40. Yuste VJ, Bayascas JR, Llecha N, Sanchez-Lopez I, Boix J, Comella JX. The absence of Oligonucleosomal DNA fragmentation during apoptosis of IMR-5 neuroblastoma cells. J Biol Chem 2001;25:22323-31.