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Volumn 12, Issue 8, 2013, Pages 1442-1452

Preclinical evaluation of the WEE1 inhibitor MK-1775 as single-agent anticancer therapy

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; CARBOPLATIN; DNA; DOXORUBICIN; MEMBRANE PROTEIN; MK 1775; MK 775; PKMYT1 PROTEIN; UNCLASSIFIED DRUG;

EID: 84882253419     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-13-0025     Document Type: Article
Times cited : (146)

References (43)
  • 1
    • 84861526824 scopus 로고    scopus 로고
    • Checkpoint control and cancer
    • Medema RH, Macurek L. Checkpoint control and cancer. Oncogene 2012;31:2601-13.
    • (2012) Oncogene , vol.31 , pp. 2601-2613
    • Medema, R.H.1    Macurek, L.2
  • 2
    • 0026616796 scopus 로고
    • Inactivation of the P34(Cdc2)-cyclin-B complex by the human WEE1 tyrosine kinase
    • Parker LL, Piwnicaworms H. Inactivation of the P34(Cdc2)-cyclin-B complex by the human WEE1 tyrosine kinase. Science 1992;257: 1955-7.
    • (1992) Science , vol.257 , pp. 1955-1957
    • Parker, L.L.1    Piwnicaworms, H.2
  • 3
    • 0029048491 scopus 로고
    • Regulation of the human WEE1Hu Cdk tyrosine 15-kinase during the cell-cycle
    • Watanabe N, Broome M, Hunter T. Regulation of the human WEE1Hu Cdk tyrosine 15-kinase during the cell-cycle. EMBO J 1995;14: 1878-91.
    • (1995) EMBO J , vol.14 , pp. 1878-1891
    • Watanabe, N.1    Broome, M.2    Hunter, T.3
  • 4
    • 79960339454 scopus 로고    scopus 로고
    • WEE1 kinase targeting combined with DNA-damaging cancer therapy catalyzes mitotic catastrophe
    • Hamer PCD, Mir SE, Noske D, Van Noorden CJF, Wurdinger T. WEE1 kinase targeting combined with DNA-damaging cancer therapy catalyzes mitotic catastrophe. Clin Cancer Res 2011;17:4200-7.
    • (2011) Clin Cancer Res , vol.17 , pp. 4200-4207
    • Hamer, P.C.D.1    Mir, S.E.2    Noske, D.3    Van Noorden, C.J.F.4    Wurdinger, T.5
  • 5
    • 0027510249 scopus 로고
    • Human WEE1 kinase inhibits cell-division by phosphorylating P34(Cdc2) exclusively on Tyr15
    • Mcgowan CH, Russell P. Human WEE1 kinase inhibits cell-division by phosphorylating P34(Cdc2) exclusively on Tyr15. EMBO J 1993;12: 75-85.
    • (1993) EMBO J , vol.12 , pp. 75-85
    • Mcgowan, C.H.1    Russell, P.2
  • 6
    • 33744905789 scopus 로고    scopus 로고
    • Murine WEE1 plays a critical role in cell cycle regulation and pre-implantation stages of embryonic development
    • Tominaga Y, Li C, Wang R-H, Deng C-X. Murine WEE1 plays a critical role in cell cycle regulation and pre-implantation stages of embryonic development. Int J Biol Sci 2006;2:161-70.
    • (2006) Int J Biol Sci , vol.2 , pp. 161-170
    • Tominaga, Y.1    Li, C.2    Wang, R.-H.3    Deng, C.-X.4
  • 7
    • 77949410508 scopus 로고    scopus 로고
    • Regulators of cyclin-dependent kinases are crucial for maintaining genome integrity in S phase
    • Beck H, Nahse V, Larsen MSY, Groth P, Clancy T, Lees M, et al. Regulators of cyclin-dependent kinases are crucial for maintaining genome integrity in S phase. J Cell Biol 2010;188:629-38.
    • (2010) J Cell Biol , vol.188 , pp. 629-638
    • Beck, H.1    Nahse, V.2    Larsen, M.S.Y.3    Groth, P.4    Clancy, T.5    Lees, M.6
  • 9
    • 84868689115 scopus 로고    scopus 로고
    • Cyclin-dependent kinase suppression by WEE1 kinase protects the genome through control of replication initiation and nucleotide consumption
    • Beck H, Nahse-Kumpf V, Larsen MS, O'Hanlon KA, Patzke S, Holmberg C, et al. Cyclin-dependent kinase suppression by WEE1 kinase protects the genome through control of replication initiation and nucleotide consumption. Mol Cell Biol 2012;32:4226-36.
    • (2012) Mol Cell Biol , vol.32 , pp. 4226-4236
    • Beck, H.1    Nahse-Kumpf, V.2    Larsen, M.S.3    O'Hanlon, K.A.4    Patzke, S.5    Holmberg, C.6
  • 10
    • 77956517283 scopus 로고    scopus 로고
    • In silico analysis of kinase expression identifies WEE1 as a gatekeeper against mitotic catastrophe in glioblastoma
    • Mir SE, Hamer PCD, Krawczyk PM, Balaj L, Claes A, Niers JM, et al. In silico analysis of kinase expression identifies WEE1 as a gatekeeper against mitotic catastrophe in glioblastoma. Cancer Cell 2010;18: 244-57.
    • (2010) Cancer Cell , vol.18 , pp. 244-257
    • Mir, S.E.1    Hamer, P.C.D.2    Krawczyk, P.M.3    Balaj, L.4    Claes, A.5    Niers, J.M.6
  • 11
    • 84862185038 scopus 로고    scopus 로고
    • High expression of WEE1 is associated with poor disease-free survival in malignant melanoma: Potential for targeted therapy
    • Magnussen GI, Holm R, Emilsen E, Rosnes AKR, Slipicevic A, Florenes VA. High expression of WEE1 is associated with poor disease-free survival in malignant melanoma: Potential for targeted therapy. PLoS One 2012;7:e38254.
    • (2012) PLoS One , vol.7
    • Magnussen, G.I.1    Holm, R.2    Emilsen, E.3    Rosnes, A.K.R.4    Slipicevic, A.5    Florenes, V.A.6
  • 12
    • 0037371056 scopus 로고    scopus 로고
    • Cyclins and cyclin-dependent kinases: Comparative study of hepatocellular carcinoma versus cirrhosis
    • Masaki T, Shiratori Y, Rengifo W, Igarashi K, Yamagata M, Kurokohchi K, et al. Cyclins and cyclin-dependent kinases: Comparative study of hepatocellular carcinoma versus cirrhosis. Hepatology 2003;37: 534-43.
    • (2003) Hepatology , vol.37 , pp. 534-543
    • Masaki, T.1    Shiratori, Y.2    Rengifo, W.3    Igarashi, K.4    Yamagata, M.5    Kurokohchi, K.6
  • 13
    • 65249161106 scopus 로고    scopus 로고
    • Integrated functional, gene expression and genomic analysis for the identification of cancer targets
    • Iorns E, Lord CJ, Grigoriadis A, McDonald S, Fenwick K, Mackay A, et al. Integrated functional, gene expression and genomic analysis for the identification of cancer targets. PLoS One 2009;4:e5120.
    • (2009) PLoS One , vol.4
    • Iorns, E.1    Lord, C.J.2    Grigoriadis, A.3    McDonald, S.4    Fenwick, K.5    Mackay, A.6
  • 14
    • 0032817385 scopus 로고    scopus 로고
    • Differential gene expression in colon carcinoma cells and tissues detected with a cDNA array
    • Backert S, Gelos M, Kobalz U, Hanski ML, Bohm C, Mann B, et al. Differential gene expression in colon carcinoma cells and tissues detected with a cDNA array. Int J Cancer 1999;82:868-74.
    • (1999) Int J Cancer , vol.82 , pp. 868-874
    • Backert, S.1    Gelos, M.2    Kobalz, U.3    Hanski, M.L.4    Bohm, C.5    Mann, B.6
  • 15
    • 1342267616 scopus 로고    scopus 로고
    • The clinical significance of Cyclin B1 and WEE1 expression in non-small-cell lung cancer
    • Yoshida T, Tanaka S, Mogi A, Shitara Y, Kuwano H. The clinical significance of Cyclin B1 and WEE1 expression in non-small-cell lung cancer. Ann Oncol 2004;15:252-6.
    • (2004) Ann Oncol , vol.15 , pp. 252-256
    • Yoshida, T.1    Tanaka, S.2    Mogi, A.3    Shitara, Y.4    Kuwano, H.5
  • 17
    • 84855908936 scopus 로고    scopus 로고
    • Safeguarding genome integrity: The checkpoint kinases ATR, CHK1 and WEE1 restrain CDK activity during normal DNA replication
    • Sorensen CS, Syljuasen RG. Safeguarding genome integrity: The checkpoint kinases ATR, CHK1 and WEE1 restrain CDK activity during normal DNA replication. Nucleic Acids Res 2012;40:477-86.
    • (2012) Nucleic Acids Res , vol.40 , pp. 477-486
    • Sorensen, C.S.1    Syljuasen, R.G.2
  • 18
    • 70949083026 scopus 로고    scopus 로고
    • Small-molecule inhibition of WEE1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents
    • Hirai H, Iwasawa Y, Okada M, Arai T, Nishibata T, Kobayashi M, et al. Small-molecule inhibition of WEE1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol Cancer Ther 2009;8:2992-3000.
    • (2009) Mol Cancer Ther , vol.8 , pp. 2992-3000
    • Hirai, H.1    Iwasawa, Y.2    Okada, M.3    Arai, T.4    Nishibata, T.5    Kobayashi, M.6
  • 19
    • 79952117003 scopus 로고    scopus 로고
    • Targeting WEE1-like protein kinase to treat cancer
    • Stathis A, Oza A. Targeting WEE1-like protein kinase to treat cancer. Drug News Perspect 2010;23:425-9.
    • (2010) Drug News Perspect , vol.23 , pp. 425-429
    • Stathis, A.1    Oza, A.2
  • 20
    • 84870656455 scopus 로고    scopus 로고
    • Update on a phase I pharmacologic and pharmacodynamic study of MK-1775, a WEE1 tyrosine kinase inhibitor, in monotherapy and combinationwith gemcitabine, cisplatin, or carboplatin in patientswith advanced solid tumors (2011 ASCO Annual Meeting)
    • (suppl; abstr 3068)
    • Schellens JHM, Shapiro G, Pavlick AC, Tibes R, Leijen S, Tolaney SM, et al. Update on a phase I pharmacologic and pharmacodynamic study of MK-1775, a WEE1 tyrosine kinase inhibitor, in monotherapy and combinationwith gemcitabine, cisplatin, or carboplatin in patientswith advanced solid tumors (2011 ASCO Annual Meeting). J Clin Oncol 29:2011, 2011 (suppl; abstr 3068).
    • (2011) J Clin Oncol , vol.29 , pp. 2011
    • Schellens, J.H.M.1    Shapiro, G.2    Pavlick, A.C.3    Tibes, R.4    Leijen, S.5    Tolaney, S.M.6
  • 21
    • 84872533885 scopus 로고    scopus 로고
    • Combination therapy targeting the Chk1 and WEE1 kinases shows therapeutic efficacy in neuroblastoma
    • Russell MR, Levin K, Rader J, Belcastro L, Li Y, Martinez D, et al. Combination therapy targeting the Chk1 and WEE1 kinases shows therapeutic efficacy in neuroblastoma. Cancer Res 2013;73:776-84.
    • (2013) Cancer Res , vol.73 , pp. 776-784
    • Russell, M.R.1    Levin, K.2    Rader, J.3    Belcastro, L.4    Li, Y.5    Martinez, D.6
  • 22
    • 17644432403 scopus 로고    scopus 로고
    • Chk1 is an essential kinase that is regulated by Atr and required for the G (2)/M DNA damage checkpoint
    • Liu Q, Guntuku S, Cui XS, Matsuoka S, Cortez D, Tamai K, et al. Chk1 is an essential kinase that is regulated by Atr and required for the G(2)/M DNA damage checkpoint. Genes Dev 2000;14:1448-59.
    • (2000) Genes Dev , vol.14 , pp. 1448-1459
    • Liu, Q.1    Guntuku, S.2    Cui, X.S.3    Matsuoka, S.4    Cortez, D.5    Tamai, K.6
  • 23
    • 0032489520 scopus 로고    scopus 로고
    • DNA doublestranded breaks induce histone H2AX phosphorylation on serine 139
    • Rogakou EP, Pilch DR, Orr AH, Ivanova VS, Bonner WM. DNA doublestranded breaks induce histone H2AX phosphorylation on serine 139. J Biol Chem 1998;273:5858-68.
    • (1998) J Biol Chem , vol.273 , pp. 5858-5868
    • Rogakou, E.P.1    Pilch, D.R.2    Orr, A.H.3    Ivanova, V.S.4    Bonner, W.M.5
  • 24
    • 0017853206 scopus 로고
    • Histone phosphorylation and chromatin structure during mitosis in Chinese hamster cells
    • Gurley LR, D'Anna JA, Barham SS, Deaven LL, Tobey RA. Histone phosphorylation and chromatin structure during mitosis in Chinese hamster cells. Eur J Biochem 1978;84:1-15.
    • (1978) Eur J Biochem , vol.84 , pp. 1-15
    • Gurley, L.R.1    D'Anna, J.A.2    Barham, S.S.3    Deaven, L.L.4    Tobey, R.A.5
  • 25
    • 0020479077 scopus 로고
    • Phosphorylation of histones 1 and 3 and nonhistone high mobility group 14 by an endogenous kinase in HeLa metaphase chromosomes
    • Paulson JR, Taylor SS. Phosphorylation of histones 1 and 3 and nonhistone high mobility group 14 by an endogenous kinase in HeLa metaphase chromosomes. J Biol Chem 1982;257:6064-72.
    • (1982) J Biol Chem , vol.257 , pp. 6064-6072
    • Paulson, J.R.1    Taylor, S.S.2
  • 26
    • 0028783413 scopus 로고
    • Myt1-A membrane-associated inhibitory kinase that phosphorylates Cdc2 on both threonine-14 and tyrosine-15
    • Mueller PR, Coleman TR, Kumagai A, Dunphy WG. Myt1-A membrane-associated inhibitory kinase that phosphorylates Cdc2 on both threonine-14 and tyrosine-15. Science 1995;270:86-90.
    • (1995) Science , vol.270 , pp. 86-90
    • Mueller, P.R.1    Coleman, T.R.2    Kumagai, A.3    Dunphy, W.G.4
  • 27
    • 84882281281 scopus 로고    scopus 로고
    • Broad Institute. Available From: Accessed May 2012
    • Broad Institute. Available from: Http://www.broadinstitute.org/ccle/home. Accessed May 2012.
  • 28
    • 67649710471 scopus 로고    scopus 로고
    • Discovery of gene expression-based pharmacodynamic biomarker for a p53 context-specific anti-tumor drug WEE1 inhibitor
    • Mizuarai S, Yamanaka K, Itadani H, Arai T, Nishibata T, Hirai H, et al. Discovery of gene expression-based pharmacodynamic biomarker for a p53 context-specific anti-tumor drug WEE1 inhibitor. Mol Cancer 2009;8:34.
    • (2009) Mol Cancer , vol.8 , pp. 34
    • Mizuarai, S.1    Yamanaka, K.2    Itadani, H.3    Arai, T.4    Nishibata, T.5    Hirai, H.6
  • 29
    • 77953711939 scopus 로고    scopus 로고
    • MK-1775, a small molecule WEE1 inhibitor, enhances antitumor efficacy of various DNA-damaging agents, including 5-fluorouracil
    • Hirai H, Arai T, Okada M, Nishibata T, Kobayashi M, Sakai N, et al. MK-1775, a small molecule WEE1 inhibitor, enhances antitumor efficacy of various DNA-damaging agents, including 5-fluorouracil. Cancer Biol Ther 2010;9:514-22.
    • (2010) Cancer Biol Ther , vol.9 , pp. 514-522
    • Hirai, H.1    Arai, T.2    Okada, M.3    Nishibata, T.4    Kobayashi, M.5    Sakai, N.6
  • 31
    • 77953726033 scopus 로고    scopus 로고
    • Targeting the checkpoint kinase WEE1 Selective sensitization of cancer cells to DNA-damaging drugs
    • Indovina P, Giordano A. Targeting the checkpoint kinase WEE1 Selective sensitization of cancer cells to DNA-damaging drugs. Cancer Biol Ther 2010;9:523-5.
    • (2010) Cancer Biol Ther , vol.9 , pp. 523-525
    • Indovina, P.1    Giordano, A.2
  • 32
    • 16544392882 scopus 로고    scopus 로고
    • Knockdown of Chk1, WEE1 and Myt1 by RNA interference abrogates G (2) checkpoint and induces apoptosis
    • Wang YL, Decker SJ, Sebolt-Leopold J. Knockdown of Chk1, WEE1 and Myt1 by RNA interference abrogates G(2) checkpoint and induces apoptosis. Cancer Biol Ther 2004;3:305-13.
    • (2004) Cancer Biol Ther , vol.3 , pp. 305-313
    • Wang, Y.L.1    Decker, S.J.2    Sebolt-Leopold, J.3
  • 33
    • 77955655940 scopus 로고    scopus 로고
    • Identification of WEE1 as a potential molecular target in cancer cells by RNAi screening of the human tyrosine kinome
    • Murrow LM, Garimella SV, Jones TL, Caplen NJ, Lipkowitz S. Identification of WEE1 as a potential molecular target in cancer cells by RNAi screening of the human tyrosine kinome. Breast Cancer Res Treat 2010;122:347-57.
    • (2010) Breast Cancer Res Treat , vol.122 , pp. 347-357
    • Murrow, L.M.1    Garimella, S.V.2    Jones, T.L.3    Caplen, N.J.4    Lipkowitz, S.5
  • 34
    • 84855645086 scopus 로고    scopus 로고
    • MK1775, a selective WEE1 inhibitor, shows single-agent antitumor activity against sarcoma cells
    • Kreahling JM, Gemmer JY, Reed D, Letson D, Bui M, Altiok S. MK1775, a selective WEE1 inhibitor, shows single-agent antitumor activity against sarcoma cells. Mol Cancer Ther 2012;11:174-82.
    • (2012) Mol Cancer Ther , vol.11 , pp. 174-182
    • Kreahling, J.M.1    Gemmer, J.Y.2    Reed, D.3    Letson, D.4    Bui, M.5    Altiok, S.6
  • 35
    • 83055187811 scopus 로고    scopus 로고
    • Novel insights into maintaining genomic integrity: WEE1 regulating Mus81/Eme1
    • Martin Y, Dominguez-Kelly R, Freire R. Novel insights into maintaining genomic integrity: WEE1 regulating Mus81/Eme1. Cell Div 2011;6:21.
    • (2011) Cell Div , vol.6 , pp. 21
    • Martin, Y.1    Dominguez-Kelly, R.2    Freire, R.3
  • 37
    • 33749053416 scopus 로고    scopus 로고
    • Identification of both Myt-1 and Wee-1 as necessary mediators of the p21-independent inactivation of the Cdc-2/cyclin B1 complex and growth inhibition of TRAMP cancer cells by genistein
    • El Touny LH, Banerjee PP. Identification of both Myt-1 and Wee-1 as necessary mediators of the p21-independent inactivation of the Cdc-2/cyclin B1 complex and growth inhibition of TRAMP cancer cells by genistein. Prostate 2006;66:1542-55.
    • (2006) Prostate , vol.66 , pp. 1542-1555
    • El Touny, L.H.1    Banerjee, P.P.2
  • 38
    • 0033067558 scopus 로고    scopus 로고
    • Overproduction of human Myt1 kinase induces a G (2) cell cycle delay by interfering with the intracellular trafficking of Cdc2-cyclin B1 complexes
    • Liu F, Rothblum-Oviatt C, Ryan CE, Piwnica-Worms H. Overproduction of human Myt1 kinase induces a G(2) cell cycle delay by interfering with the intracellular trafficking of Cdc2-cyclin B1 complexes. Mol Cell Biol 1999;19:5113-23.
    • (1999) Mol Cell Biol , vol.19 , pp. 5113-5123
    • Liu, F.1    Rothblum-Oviatt, C.2    Ryan, C.E.3    Piwnica-Worms, H.4
  • 39
    • 79955492036 scopus 로고    scopus 로고
    • MK-1775, a potent WEE1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts
    • Rajeshkumar NV, De Oliveira E, Ottenhof N, Watters J, Brooks D, Demuth T, et al. MK-1775, a potent WEE1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts. Clin Cancer Res 2011;17: 2799-806.
    • (2011) Clin Cancer Res , vol.17 , pp. 2799-2806
    • Rajeshkumar, N.V.1    De Oliveira, E.2    Ottenhof, N.3    Watters, J.4    Brooks, D.5    Demuth, T.6
  • 41
    • 84863799519 scopus 로고    scopus 로고
    • Combined inhibition of Chk1 and WEE1 in vitro synergistic effect translates to tumor growth inhibition in vivo
    • Carrassa L, Chila R, Lupi M, Ricci F, Celenza C, Mazzoletti M, et al. Combined inhibition of Chk1 and WEE1 in vitro synergistic effect translates to tumor growth inhibition in vivo. Cell Cycle 2012;11: 2507-17.
    • (2012) Cell Cycle , vol.11 , pp. 2507-2517
    • Carrassa, L.1    Chila, R.2    Lupi, M.3    Ricci, F.4    Celenza, C.5    Mazzoletti, M.6
  • 42
    • 80051887747 scopus 로고    scopus 로고
    • Single-agent inhibition of Chk1 is antiproliferative in human cancer cell lines in vitro and inhibits tumor xenograft growth in vivo
    • Davies KD, Humphries MJ, Sullivan FX, von Carlowitz I, Le Huerou Y, Mohr PJ, et al. Single-agent inhibition of Chk1 is antiproliferative in human cancer cell lines in vitro and inhibits tumor xenograft growth in vivo. Oncol Res 2011;19:349-63.
    • (2011) Oncol Res , vol.19 , pp. 349-363
    • Davies, K.D.1    Humphries, M.J.2    Sullivan, F.X.3    Von Carlowitz, I.4    Le Huerou, Y.5    Mohr, P.J.6
  • 43
    • 84868654250 scopus 로고    scopus 로고
    • Unique functions of CHK1 and WEE1 underlie synergistic anti-tumor activity upon pharmacologic inhibition
    • Guertin AD, Martin MM, Roberts B, Hurd M, Qu X, Miselis NR, et al. Unique functions of CHK1 and WEE1 underlie synergistic anti-tumor activity upon pharmacologic inhibition. Cancer Cell Int 2012;12:45.
    • (2012) Cancer Cell Int , vol.12 , pp. 45
    • Guertin, A.D.1    Martin, M.M.2    Roberts, B.3    Hurd, M.4    Qu, X.5    Miselis, N.R.6


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