메뉴 건너뛰기




Volumn 12, Issue 1, 2013, Pages

Cell cycle-dependent activity of the novel dual PI3K-MTORC1/2 inhibitor NVP-BGT226 in acute leukemia

Author keywords

AKT; Leukemia; NVP BEZ235; NVP BGT226; PI3K

Indexed keywords

1 (1 CYANO 1 METHYLETHYL) 3 METHYL 8 (3 QUINOLINYL)IMIDAZO[4,5 C]QUINOLIN 2(1H,3H) ONE; 2 MORPHOLINO 8 PHENYLCHROMONE; ANTINEOPLASTIC AGENT; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; NVP BGT 226; PROTEIN KINASE B; UNCLASSIFIED DRUG;

EID: 84878006322     PISSN: None     EISSN: 14764598     Source Type: Journal    
DOI: 10.1186/1476-4598-12-46     Document Type: Article
Times cited : (50)

References (56)
  • 1
    • 2142819411 scopus 로고    scopus 로고
    • Acute lymphoblastic leukemia
    • 10.1056/NEJMra023001, 15071128
    • Pui CH, Relling MV, Downing JR. Acute lymphoblastic leukemia. N Engl J Med 2004, 350:1535-1548. 10.1056/NEJMra023001, 15071128.
    • (2004) N Engl J Med , vol.350 , pp. 1535-1548
    • Pui, C.H.1    Relling, M.V.2    Downing, J.R.3
  • 2
    • 77449159028 scopus 로고    scopus 로고
    • Diagnosis and management of acute myeloid leukemia in adults: recommendations from an international expert panel, on behalf of the European LeukemiaNet
    • 10.1182/blood-2009-07-235358, 19880497
    • Dohner H, Estey EH, Amadori S, Appelbaum FR, Buchner T, Burnett AK, Dombret H, Fenaux P, Grimwade D, Larson RA. Diagnosis and management of acute myeloid leukemia in adults: recommendations from an international expert panel, on behalf of the European LeukemiaNet. Blood 2010, 115:453-474. 10.1182/blood-2009-07-235358, 19880497.
    • (2010) Blood , vol.115 , pp. 453-474
    • Dohner, H.1    Estey, E.H.2    Amadori, S.3    Appelbaum, F.R.4    Buchner, T.5    Burnett, A.K.6    Dombret, H.7    Fenaux, P.8    Grimwade, D.9    Larson, R.A.10
  • 3
    • 0035810142 scopus 로고    scopus 로고
    • Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome
    • 10.1056/NEJM200104053441402, 11287973
    • Druker BJ, Sawyers CL, Kantarjian H, Resta DJ, Reese SF, Ford JM, Capdeville R, Talpaz M. Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome. N Engl J Med 2001, 344:1038-1042. 10.1056/NEJM200104053441402, 11287973.
    • (2001) N Engl J Med , vol.344 , pp. 1038-1042
    • Druker, B.J.1    Sawyers, C.L.2    Kantarjian, H.3    Resta, D.J.4    Reese, S.F.5    Ford, J.M.6    Capdeville, R.7    Talpaz, M.8
  • 4
    • 0037648683 scopus 로고    scopus 로고
    • Complete remission of third recurrence of acute myeloid leukemia after treatment with imatinib (STI-571)
    • 10.1080/1042819031000077034, 12916883
    • Schittenhelm M, Aichele O, Krober SM, Brummendorf T, Kanz L, Denzlinger C. Complete remission of third recurrence of acute myeloid leukemia after treatment with imatinib (STI-571). Leuk Lymphoma 2003, 44:1251-1253. 10.1080/1042819031000077034, 12916883.
    • (2003) Leuk Lymphoma , vol.44 , pp. 1251-1253
    • Schittenhelm, M.1    Aichele, O.2    Krober, S.M.3    Brummendorf, T.4    Kanz, L.5    Denzlinger, C.6
  • 5
    • 0037606031 scopus 로고    scopus 로고
    • Sustained complete hematologic remission after administration of the tyrosine kinase inhibitor imatinib mesylate in a patient with refractory, secondary AML
    • 10.1182/blood-2002-05-1469, 12480706
    • Kindler T, Breitenbuecher F, Marx A, Hess G, Gschaidmeier H, Gamm H, Kirkpatrick CJ, Huber C, Fischer T. Sustained complete hematologic remission after administration of the tyrosine kinase inhibitor imatinib mesylate in a patient with refractory, secondary AML. Blood 2003, 101:2960-2962. 10.1182/blood-2002-05-1469, 12480706.
    • (2003) Blood , vol.101 , pp. 2960-2962
    • Kindler, T.1    Breitenbuecher, F.2    Marx, A.3    Hess, G.4    Gschaidmeier, H.5    Gamm, H.6    Kirkpatrick, C.J.7    Huber, C.8    Fischer, T.9
  • 7
    • 78650073854 scopus 로고    scopus 로고
    • FLT3 as a therapeutic target in AML: still challenging after all these years
    • 10.1182/blood-2010-04-261867, 20705759
    • Kindler T, Lipka DB, Fischer T. FLT3 as a therapeutic target in AML: still challenging after all these years. Blood 2010, 116:5089-5102. 10.1182/blood-2010-04-261867, 20705759.
    • (2010) Blood , vol.116 , pp. 5089-5102
    • Kindler, T.1    Lipka, D.B.2    Fischer, T.3
  • 8
    • 34250788809 scopus 로고    scopus 로고
    • AKT/PKB signaling: navigating downstream
    • 10.1016/j.cell.2007.06.009, 2756685, 17604717
    • Manning BD, Cantley LC. AKT/PKB signaling: navigating downstream. Cell 2007, 129:1261-1274. 10.1016/j.cell.2007.06.009, 2756685, 17604717.
    • (2007) Cell , vol.129 , pp. 1261-1274
    • Manning, B.D.1    Cantley, L.C.2
  • 9
    • 77949900650 scopus 로고    scopus 로고
    • Constitutively active AKT depletes hematopoietic stem cells and induces leukemia in mice
    • 10.1182/blood-2009-06-229443, 2826762, 20008787
    • Kharas MG, Okabe R, Ganis JJ, Gozo M, Khandan T, Paktinat M, Gilliland DG, Gritsman K. Constitutively active AKT depletes hematopoietic stem cells and induces leukemia in mice. Blood 2010, 115:1406-1415. 10.1182/blood-2009-06-229443, 2826762, 20008787.
    • (2010) Blood , vol.115 , pp. 1406-1415
    • Kharas, M.G.1    Okabe, R.2    Ganis, J.J.3    Gozo, M.4    Khandan, T.5    Paktinat, M.6    Gilliland, D.G.7    Gritsman, K.8
  • 10
    • 27544450742 scopus 로고    scopus 로고
    • Constitutive activation of Akt by Flt3 internal tandem duplications is necessary for increased survival, proliferation, and myeloid transformation
    • 10.1158/0008-5472.CAN-05-0422, 16266983
    • Brandts CH, Sargin B, Rode M, Biermann C, Lindtner B, Schwable J, Buerger H, Muller-Tidow C, Choudhary C, McMahon M. Constitutive activation of Akt by Flt3 internal tandem duplications is necessary for increased survival, proliferation, and myeloid transformation. Cancer Res 2005, 65:9643-9650. 10.1158/0008-5472.CAN-05-0422, 16266983.
    • (2005) Cancer Res , vol.65 , pp. 9643-9650
    • Brandts, C.H.1    Sargin, B.2    Rode, M.3    Biermann, C.4    Lindtner, B.5    Schwable, J.6    Buerger, H.7    Muller-Tidow, C.8    Choudhary, C.9    McMahon, M.10
  • 11
    • 0035872199 scopus 로고    scopus 로고
    • Akt/protein kinase B is constitutively active in non-small cell lung cancer cells and promotes cellular survival and resistance to chemotherapy and radiation
    • Brognard J, Clark AS, Ni Y, Dennis PA. Akt/protein kinase B is constitutively active in non-small cell lung cancer cells and promotes cellular survival and resistance to chemotherapy and radiation. Cancer Res 2001, 61:3986-3997.
    • (2001) Cancer Res , vol.61 , pp. 3986-3997
    • Brognard, J.1    Clark, A.S.2    Ni, Y.3    Dennis, P.A.4
  • 12
    • 0036632368 scopus 로고    scopus 로고
    • The phosphatidylinositol 3-Kinase AKT pathway in human cancer
    • 10.1038/nrc839, 12094235
    • Vivanco I, Sawyers CL. The phosphatidylinositol 3-Kinase AKT pathway in human cancer. Nat Rev Cancer 2002, 2:489-501. 10.1038/nrc839, 12094235.
    • (2002) Nat Rev Cancer , vol.2 , pp. 489-501
    • Vivanco, I.1    Sawyers, C.L.2
  • 14
    • 43249115083 scopus 로고    scopus 로고
    • Mutational analysis of oncogenic AKT E17K mutation in common solid cancers and acute leukaemias
    • 10.1038/sj.bjc.6604212, 2391109, 18392055
    • Kim MS, Jeong EG, Yoo NJ, Lee SH. Mutational analysis of oncogenic AKT E17K mutation in common solid cancers and acute leukaemias. Br J Cancer 2008, 98:1533-1535. 10.1038/sj.bjc.6604212, 2391109, 18392055.
    • (2008) Br J Cancer , vol.98 , pp. 1533-1535
    • Kim, M.S.1    Jeong, E.G.2    Yoo, N.J.3    Lee, S.H.4
  • 15
    • 79953038262 scopus 로고    scopus 로고
    • PTEN loss in the continuum of common cancers, rare syndromes and mouse models
    • Hollander MC, Blumenthal GM, Dennis PA. PTEN loss in the continuum of common cancers, rare syndromes and mouse models. Nat Rev Cancer 2011, 11:289-301.
    • (2011) Nat Rev Cancer , vol.11 , pp. 289-301
    • Hollander, M.C.1    Blumenthal, G.M.2    Dennis, P.A.3
  • 16
    • 65949086609 scopus 로고    scopus 로고
    • PTEN loss contributes to erlotinib resistance in EGFR-mutant lung cancer by activation of Akt and EGFR
    • 10.1158/0008-5472.CAN-08-4055, 2849653, 19351834
    • Sos ML, Koker M, Weir BA, Heynck S, Rabinovsky R, Zander T, Seeger JM, Weiss J, Fischer F, Frommolt P. PTEN loss contributes to erlotinib resistance in EGFR-mutant lung cancer by activation of Akt and EGFR. Cancer Res 2009, 69:3256-3261. 10.1158/0008-5472.CAN-08-4055, 2849653, 19351834.
    • (2009) Cancer Res , vol.69 , pp. 3256-3261
    • Sos, M.L.1    Koker, M.2    Weir, B.A.3    Heynck, S.4    Rabinovsky, R.5    Zander, T.6    Seeger, J.M.7    Weiss, J.8    Fischer, F.9    Frommolt, P.10
  • 17
    • 43449092194 scopus 로고    scopus 로고
    • Chronic lymphocytic leukaemia and acute myeloid leukaemia are not associated with AKT1 pleckstrin homology domain (E17K) mutations
    • 10.1111/j.1365-2141.2008.07113.x, 18410456
    • Zenz T, Dohner K, Denzel T, Dohner H, Stilgenbauer S, Bullinger L. Chronic lymphocytic leukaemia and acute myeloid leukaemia are not associated with AKT1 pleckstrin homology domain (E17K) mutations. Br J Haematol 2008, 141:742-743. 10.1111/j.1365-2141.2008.07113.x, 18410456.
    • (2008) Br J Haematol , vol.141 , pp. 742-743
    • Zenz, T.1    Dohner, K.2    Denzel, T.3    Dohner, H.4    Stilgenbauer, S.5    Bullinger, L.6
  • 18
    • 38349086652 scopus 로고    scopus 로고
    • PI3K/AKT pathway activation in acute myeloid leukaemias is not associated with AKT1 pleckstrin homology domain mutation
    • 10.1111/j.1365-2141.2007.06920.x, 3385948, 18053070
    • Tibes R, Kornblau SM, Qiu Y, Mousses SM, Robbins C, Moses T, Carpten JD. PI3K/AKT pathway activation in acute myeloid leukaemias is not associated with AKT1 pleckstrin homology domain mutation. Br J Haematol 2008, 140:344-347. 10.1111/j.1365-2141.2007.06920.x, 3385948, 18053070.
    • (2008) Br J Haematol , vol.140 , pp. 344-347
    • Tibes, R.1    Kornblau, S.M.2    Qiu, Y.3    Mousses, S.M.4    Robbins, C.5    Moses, T.6    Carpten, J.D.7
  • 19
    • 33744457653 scopus 로고    scopus 로고
    • Phosphoinositide 3-kinase/Akt signaling pathway and its therapeutical implications for human acute myeloid leukemia
    • 10.1038/sj.leu.2404245, 16642045
    • Martelli AM, Nyakern M, Tabellini G, Bortul R, Tazzari PL, Evangelisti C, Cocco L. Phosphoinositide 3-kinase/Akt signaling pathway and its therapeutical implications for human acute myeloid leukemia. Leukemia 2006, 20:911-928. 10.1038/sj.leu.2404245, 16642045.
    • (2006) Leukemia , vol.20 , pp. 911-928
    • Martelli, A.M.1    Nyakern, M.2    Tabellini, G.3    Bortul, R.4    Tazzari, P.L.5    Evangelisti, C.6    Cocco, L.7
  • 20
    • 79952109693 scopus 로고    scopus 로고
    • From the bench to the bed side: PI3K pathway inhibitors in clinical development
    • 10.1007/82_2010_60, 20582534
    • Maira SM, Finan P, Garcia-Echeverria C. From the bench to the bed side: PI3K pathway inhibitors in clinical development. Curr Top Microbiol Immunol 2010, 347:209-239. 10.1007/82_2010_60, 20582534.
    • (2010) Curr Top Microbiol Immunol , vol.347 , pp. 209-239
    • Maira, S.M.1    Finan, P.2    Garcia-Echeverria, C.3
  • 24
    • 38049187096 scopus 로고    scopus 로고
    • Mammalian target of rapamycin (mTOR) inhibition activates phosphatidylinositol 3-kinase/Akt by up-regulating insulin-like growth factor-1 receptor signaling in acute myeloid leukemia: rationale for therapeutic inhibition of both pathways
    • 10.1182/blood-2007-03-080796, 17878402
    • Tamburini J, Chapuis N, Bardet V, Park S, Sujobert P, Willems L, Ifrah N, Dreyfus F, Mayeux P, Lacombe C, Bouscary D. Mammalian target of rapamycin (mTOR) inhibition activates phosphatidylinositol 3-kinase/Akt by up-regulating insulin-like growth factor-1 receptor signaling in acute myeloid leukemia: rationale for therapeutic inhibition of both pathways. Blood 2008, 111:379-382. 10.1182/blood-2007-03-080796, 17878402.
    • (2008) Blood , vol.111 , pp. 379-382
    • Tamburini, J.1    Chapuis, N.2    Bardet, V.3    Park, S.4    Sujobert, P.5    Willems, L.6    Ifrah, N.7    Dreyfus, F.8    Mayeux, P.9    Lacombe, C.10    Bouscary, D.11
  • 26
  • 27
    • 81255129000 scopus 로고    scopus 로고
    • Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo
    • 10.1158/1078-0432.CCR-11-0796, 21976531
    • Chang KY, Tsai SY, Wu CM, Yen CJ, Chuang BF, Chang JY. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res 2011, 17:7116-7126. 10.1158/1078-0432.CCR-11-0796, 21976531.
    • (2011) Clin Cancer Res , vol.17 , pp. 7116-7126
    • Chang, K.Y.1    Tsai, S.Y.2    Wu, C.M.3    Yen, C.J.4    Chuang, B.F.5    Chang, J.Y.6
  • 28
    • 51049109033 scopus 로고    scopus 로고
    • Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
    • 10.1158/1535-7163.MCT-08-0017, 18606717
    • Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chene P, De Pover A, Schoemaker K. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther 2008, 7:1851-1863. 10.1158/1535-7163.MCT-08-0017, 18606717.
    • (2008) Mol Cancer Ther , vol.7 , pp. 1851-1863
    • Maira, S.M.1    Stauffer, F.2    Brueggen, J.3    Furet, P.4    Schnell, C.5    Fritsch, C.6    Brachmann, S.7    Chene, P.8    De Pover, A.9    Schoemaker, K.10
  • 29
    • 84856244294 scopus 로고    scopus 로고
    • The PI3K/PKB signaling module as key regulator of hematopoiesis: implications for therapeutic strategies in leukemia
    • 10.1182/blood-2011-07-366203, 22065598
    • Polak R, Buitenhuis M. The PI3K/PKB signaling module as key regulator of hematopoiesis: implications for therapeutic strategies in leukemia. Blood 2012, 119:911-923. 10.1182/blood-2011-07-366203, 22065598.
    • (2012) Blood , vol.119 , pp. 911-923
    • Polak, R.1    Buitenhuis, M.2
  • 30
    • 67349180268 scopus 로고    scopus 로고
    • The level of AKT phosphorylation on threonine 308 but not on serine 473 is associated with high-risk cytogenetics and predicts poor overall survival in acute myeloid leukaemia
    • 10.1038/leu.2008.395, 19158829
    • Gallay N, Dos Santos C, Cuzin L, Bousquet M, Simmonet Gouy V, Chaussade C, Attal M, Payrastre B, Demur C, Recher C. The level of AKT phosphorylation on threonine 308 but not on serine 473 is associated with high-risk cytogenetics and predicts poor overall survival in acute myeloid leukaemia. Leukemia 2009, 23:1029-1038. 10.1038/leu.2008.395, 19158829.
    • (2009) Leukemia , vol.23 , pp. 1029-1038
    • Gallay, N.1    Dos Santos, C.2    Cuzin, L.3    Bousquet, M.4    Simmonet Gouy, V.5    Chaussade, C.6    Attal, M.7    Payrastre, B.8    Demur, C.9    Recher, C.10
  • 31
    • 0033811659 scopus 로고    scopus 로고
    • Deficiency of PTEN in Jurkat T cells causes constitutive localization of Itk to the plasma membrane and hyperresponsiveness to CD3 stimulation
    • 10.1128/MCB.20.18.6945-6957.2000, 88770, 10958690
    • Shan X, Czar MJ, Bunnell SC, Liu P, Liu Y, Schwartzberg PL, Wange RL. Deficiency of PTEN in Jurkat T cells causes constitutive localization of Itk to the plasma membrane and hyperresponsiveness to CD3 stimulation. Mol Cell Biol 2000, 20:6945-6957. 10.1128/MCB.20.18.6945-6957.2000, 88770, 10958690.
    • (2000) Mol Cell Biol , vol.20 , pp. 6945-6957
    • Shan, X.1    Czar, M.J.2    Bunnell, S.C.3    Liu, P.4    Liu, Y.5    Schwartzberg, P.L.6    Wange, R.L.7
  • 32
    • 78349273297 scopus 로고    scopus 로고
    • Dual inhibition of PI3K and mTORC1/2 signaling by NVP-BEZ235 as a new therapeutic strategy for acute myeloid leukemia
    • 10.1158/1078-0432.CCR-10-1102, 20884625
    • Chapuis N, Tamburini J, Green AS, Vignon C, Bardet V, Neyret A, Pannetier M, Willems L, Park S, Macone A. Dual inhibition of PI3K and mTORC1/2 signaling by NVP-BEZ235 as a new therapeutic strategy for acute myeloid leukemia. Clin Cancer Res 2010, 16:5424-5435. 10.1158/1078-0432.CCR-10-1102, 20884625.
    • (2010) Clin Cancer Res , vol.16 , pp. 5424-5435
    • Chapuis, N.1    Tamburini, J.2    Green, A.S.3    Vignon, C.4    Bardet, V.5    Neyret, A.6    Pannetier, M.7    Willems, L.8    Park, S.9    Macone, A.10
  • 33
    • 0842304369 scopus 로고    scopus 로고
    • Mammalian target of rapamycin inhibition as therapy for hematologic malignancies
    • 10.1002/cncr.20026, 14770419
    • Panwalkar A, Verstovsek S, Giles FJ. Mammalian target of rapamycin inhibition as therapy for hematologic malignancies. Cancer 2004, 100:657-666. 10.1002/cncr.20026, 14770419.
    • (2004) Cancer , vol.100 , pp. 657-666
    • Panwalkar, A.1    Verstovsek, S.2    Giles, F.J.3
  • 34
    • 81155123729 scopus 로고    scopus 로고
    • The serine/threonine kinase ULK1 is a target of multiple phosphorylation events
    • 10.1042/BJ20101894, 21819378
    • Bach M, Larance M, James DE, Ramm G. The serine/threonine kinase ULK1 is a target of multiple phosphorylation events. Biochem J 2011, 440:283-291. 10.1042/BJ20101894, 21819378.
    • (2011) Biochem J , vol.440 , pp. 283-291
    • Bach, M.1    Larance, M.2    James, D.E.3    Ramm, G.4
  • 35
    • 31544459272 scopus 로고    scopus 로고
    • Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies
    • 10.1158/0008-5472.CAN-05-2050, 16397263
    • Schittenhelm MM, Shiraga S, Schroeder A, Corbin AS, Griffith D, Lee FY, Bokemeyer C, Deininger MW, Druker BJ, Heinrich MC. Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res 2006, 66:473-481. 10.1158/0008-5472.CAN-05-2050, 16397263.
    • (2006) Cancer Res , vol.66 , pp. 473-481
    • Schittenhelm, M.M.1    Shiraga, S.2    Schroeder, A.3    Corbin, A.S.4    Griffith, D.5    Lee, F.Y.6    Bokemeyer, C.7    Deininger, M.W.8    Druker, B.J.9    Heinrich, M.C.10
  • 36
    • 33750344194 scopus 로고    scopus 로고
    • FLT3 K663Q is a novel AML-associated oncogenic kinase: Determination of biochemical properties and sensitivity to Sunitinib (SU11248)
    • 10.1038/sj.leu.2404374, 16990784
    • Schittenhelm MM, Yee KW, Tyner JW, McGreevey L, Haley AD, Town A, Griffith DJ, Bainbridge T, Braziel RM, O'Farrell AM. FLT3 K663Q is a novel AML-associated oncogenic kinase: Determination of biochemical properties and sensitivity to Sunitinib (SU11248). Leukemia 2006, 20:2008-2014. 10.1038/sj.leu.2404374, 16990784.
    • (2006) Leukemia , vol.20 , pp. 2008-2014
    • Schittenhelm, M.M.1    Yee, K.W.2    Tyner, J.W.3    McGreevey, L.4    Haley, A.D.5    Town, A.6    Griffith, D.J.7    Bainbridge, T.8    Braziel, R.M.9    O'Farrell, A.M.10
  • 37
    • 0021118703 scopus 로고
    • Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors
    • Chou TC, Talalay P. Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv Enzyme Regul 1984, 22:27-55.
    • (1984) Adv Enzyme Regul , vol.22 , pp. 27-55
    • Chou, T.C.1    Talalay, P.2
  • 39
    • 82555166037 scopus 로고    scopus 로고
    • Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma
    • 10.1097/CAD.0b013e32834c8683, 21959532
    • Baumann P, Schneider L, Mandl-Weber S, Oduncu F, Schmidmaier R. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs 2012, 23:131-138. 10.1097/CAD.0b013e32834c8683, 21959532.
    • (2012) Anticancer Drugs , vol.23 , pp. 131-138
    • Baumann, P.1    Schneider, L.2    Mandl-Weber, S.3    Oduncu, F.4    Schmidmaier, R.5
  • 40
    • 84860747223 scopus 로고    scopus 로고
    • Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia
    • 10.1038/nature11016, 3390926, 22504184
    • Smith CC, Wang Q, Chin CS, Salerno S, Damon LE, Levis MJ, Perl AE, Travers KJ, Wang S, Hunt JP. Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia. Nature 2012, 485:260-263. 10.1038/nature11016, 3390926, 22504184.
    • (2012) Nature , vol.485 , pp. 260-263
    • Smith, C.C.1    Wang, Q.2    Chin, C.S.3    Salerno, S.4    Damon, L.E.5    Levis, M.J.6    Perl, A.E.7    Travers, K.J.8    Wang, S.9    Hunt, J.P.10
  • 41
    • 36749030022 scopus 로고    scopus 로고
    • KIT oncogenic signaling mechanisms in imatinib-resistant gastrointestinal stromal tumor: PI3-kinase/AKT is a crucial survival pathway
    • 10.1038/sj.onc.1210558, 17546049
    • Bauer S, Duensing A, Demetri GD, Fletcher JA. KIT oncogenic signaling mechanisms in imatinib-resistant gastrointestinal stromal tumor: PI3-kinase/AKT is a crucial survival pathway. Oncogene 2007, 26:7560-7568. 10.1038/sj.onc.1210558, 17546049.
    • (2007) Oncogene , vol.26 , pp. 7560-7568
    • Bauer, S.1    Duensing, A.2    Demetri, G.D.3    Fletcher, J.A.4
  • 42
    • 0027359443 scopus 로고
    • Identification of mutations in the coding sequence of the proto-oncogene c-kit in a human mast cell leukemia cell line causing ligand-independent activation of c-kit product
    • 10.1172/JCI116761, 288334, 7691885
    • Furitsu T, Tsujimura T, Tono T, Ikeda H, Kitayama H, Koshimizu U, Sugahara H, Butterfield JH, Ashman LK, Kanayama Y. Identification of mutations in the coding sequence of the proto-oncogene c-kit in a human mast cell leukemia cell line causing ligand-independent activation of c-kit product. J Clin Invest 1993, 92:1736-1744. 10.1172/JCI116761, 288334, 7691885.
    • (1993) J Clin Invest , vol.92 , pp. 1736-1744
    • Furitsu, T.1    Tsujimura, T.2    Tono, T.3    Ikeda, H.4    Kitayama, H.5    Koshimizu, U.6    Sugahara, H.7    Butterfield, J.H.8    Ashman, L.K.9    Kanayama, Y.10
  • 43
    • 0036493872 scopus 로고    scopus 로고
    • The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations
    • 10.1182/blood.V99.5.1741, 11861291
    • Ma Y, Zeng S, Metcalfe DD, Akin C, Dimitrijevic S, Butterfield JH, McMahon G, Longley BJ. The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations. Blood 2002, 99:1741-1744. 10.1182/blood.V99.5.1741, 11861291.
    • (2002) Blood , vol.99 , pp. 1741-1744
    • Ma, Y.1    Zeng, S.2    Metcalfe, D.D.3    Akin, C.4    Dimitrijevic, S.5    Butterfield, J.H.6    McMahon, G.7    Longley, B.J.8
  • 44
    • 0035899418 scopus 로고    scopus 로고
    • STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications
    • 10.1038/sj.onc.1204704, 11526490
    • Tuveson DA, Willis NA, Jacks T, Griffin JD, Singer S, Fletcher CD, Fletcher JA, Demetri GD. STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications. Oncogene 2001, 20:5054-5058. 10.1038/sj.onc.1204704, 11526490.
    • (2001) Oncogene , vol.20 , pp. 5054-5058
    • Tuveson, D.A.1    Willis, N.A.2    Jacks, T.3    Griffin, J.D.4    Singer, S.5    Fletcher, C.D.6    Fletcher, J.A.7    Demetri, G.D.8
  • 45
    • 33749461709 scopus 로고    scopus 로고
    • Heat shock protein 90 inhibition in imatinib-resistant gastrointestinal stromal tumor
    • 10.1158/0008-5472.CAN-06-0165, 16982758
    • Bauer S, Yu LK, Demetri GD, Fletcher JA. Heat shock protein 90 inhibition in imatinib-resistant gastrointestinal stromal tumor. Cancer Res 2006, 66:9153-9161. 10.1158/0008-5472.CAN-06-0165, 16982758.
    • (2006) Cancer Res , vol.66 , pp. 9153-9161
    • Bauer, S.1    Yu, L.K.2    Demetri, G.D.3    Fletcher, J.A.4
  • 47
    • 77951641594 scopus 로고    scopus 로고
    • High EVI1 expression predicts outcome in younger adult patients with acute myeloid leukemia and is associated with distinct cytogenetic abnormalities
    • 10.1200/JCO.2009.26.0646, 20308656
    • Groschel S, Lugthart S, Schlenk RF, Valk PJ, Eiwen K, Goudswaard C, van Putten WJ, Kayser S, Verdonck LF, Lubbert M. High EVI1 expression predicts outcome in younger adult patients with acute myeloid leukemia and is associated with distinct cytogenetic abnormalities. J Clin Oncol 2010, 28:2101-2107. 10.1200/JCO.2009.26.0646, 20308656.
    • (2010) J Clin Oncol , vol.28 , pp. 2101-2107
    • Groschel, S.1    Lugthart, S.2    Schlenk, R.F.3    Valk, P.J.4    Eiwen, K.5    Goudswaard, C.6    van Putten, W.J.7    Kayser, S.8    Verdonck, L.F.9    Lubbert, M.10
  • 48
    • 79953683693 scopus 로고    scopus 로고
    • Evi1 represses PTEN expression and activates PI3K/AKT/mTOR via interactions with polycomb proteins
    • 10.1182/blood-2009-12-261602, 21289308
    • Yoshimi A, Goyama S, Watanabe-Okochi N, Yoshiki Y, Nannya Y, Nitta E, Arai S, Sato T, Shimabe M, Nakagawa M. Evi1 represses PTEN expression and activates PI3K/AKT/mTOR via interactions with polycomb proteins. Blood 2011, 117:3617-3628. 10.1182/blood-2009-12-261602, 21289308.
    • (2011) Blood , vol.117 , pp. 3617-3628
    • Yoshimi, A.1    Goyama, S.2    Watanabe-Okochi, N.3    Yoshiki, Y.4    Nannya, Y.5    Nitta, E.6    Arai, S.7    Sato, T.8    Shimabe, M.9    Nakagawa, M.10
  • 50
    • 84865562515 scopus 로고    scopus 로고
    • Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors
    • 10.1093/annonc/mds011, 22357447
    • Markman B, Tabernero J, Krop I, Shapiro GI, Siu L, Chen LC, Mita M, Melendez Cuero M, Stutvoet S, Birle D. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol 2012, 23:2399-2408. 10.1093/annonc/mds011, 22357447.
    • (2012) Ann Oncol , vol.23 , pp. 2399-2408
    • Markman, B.1    Tabernero, J.2    Krop, I.3    Shapiro, G.I.4    Siu, L.5    Chen, L.C.6    Mita, M.7    Melendez Cuero, M.8    Stutvoet, S.9    Birle, D.10
  • 51
    • 84863576741 scopus 로고    scopus 로고
    • The dual PI3K/mTOR inhibitor NVP-BGT226 induces cell cycle arrest and regulates Survivin gene expression in human pancreatic cancer cell lines
    • 10.1007/s13277-011-0290-2, 22170433
    • Glienke W, Maute L, Wicht J, Bergmann L. The dual PI3K/mTOR inhibitor NVP-BGT226 induces cell cycle arrest and regulates Survivin gene expression in human pancreatic cancer cell lines. Tumour Biol 2012, 33:757-765. 10.1007/s13277-011-0290-2, 22170433.
    • (2012) Tumour Biol , vol.33 , pp. 757-765
    • Glienke, W.1    Maute, L.2    Wicht, J.3    Bergmann, L.4
  • 52
    • 0037265645 scopus 로고    scopus 로고
    • FLT3 mutations in acute myeloid leukemia cell lines
    • 10.1038/sj.leu.2402740, 12529668
    • Quentmeier H, Reinhardt J, Zaborski M, Drexler HG. FLT3 mutations in acute myeloid leukemia cell lines. Leukemia 2003, 17:120-124. 10.1038/sj.leu.2402740, 12529668.
    • (2003) Leukemia , vol.17 , pp. 120-124
    • Quentmeier, H.1    Reinhardt, J.2    Zaborski, M.3    Drexler, H.G.4
  • 53
    • 36649000489 scopus 로고    scopus 로고
    • Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles
    • 10.1016/j.ccr.2007.11.005, 18068628
    • Frohling S, Scholl C, Levine RL, Loriaux M, Boggon TJ, Bernard OA, Berger R, Dohner H, Dohner K, Ebert BL. Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles. Cancer Cell 2007, 12:501-513. 10.1016/j.ccr.2007.11.005, 18068628.
    • (2007) Cancer Cell , vol.12 , pp. 501-513
    • Frohling, S.1    Scholl, C.2    Levine, R.L.3    Loriaux, M.4    Boggon, T.J.5    Bernard, O.A.6    Berger, R.7    Dohner, H.8    Dohner, K.9    Ebert, B.L.10
  • 54
    • 10244277976 scopus 로고    scopus 로고
    • Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells
    • 10.1182/blood-2003-10-3381, 15304385
    • Yee KW, Schittenhelm M, O'Farrell AM, Town AR, McGreevey L, Bainbridge T, Cherrington JM, Heinrich MC. Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells. Blood 2004, 104:4202-4209. 10.1182/blood-2003-10-3381, 15304385.
    • (2004) Blood , vol.104 , pp. 4202-4209
    • Yee, K.W.1    Schittenhelm, M.2    O'Farrell, A.M.3    Town, A.R.4    McGreevey, L.5    Bainbridge, T.6    Cherrington, J.M.7    Heinrich, M.C.8
  • 55
    • 69249212433 scopus 로고    scopus 로고
    • The FLT3 inhibitor tandutinib (formerly MLN518) has sequence-independent synergistic effects with cytarabine and daunorubicin
    • 10.4161/cc.8.16.9355, 19625780
    • Schittenhelm MM, Kampa KM, Yee KW, Heinrich MC. The FLT3 inhibitor tandutinib (formerly MLN518) has sequence-independent synergistic effects with cytarabine and daunorubicin. Cell Cycle 2009, 8:2621-2630. 10.4161/cc.8.16.9355, 19625780.
    • (2009) Cell Cycle , vol.8 , pp. 2621-2630
    • Schittenhelm, M.M.1    Kampa, K.M.2    Yee, K.W.3    Heinrich, M.C.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.