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Volumn 74, Issue 18, 2014, Pages 5206-5217

FLT3 kinase inhibitor TTT-3002 overcomes both activating and drug resistance mutations in FLT3 in acute myeloid leukemia

Author keywords

[No Author keywords available]

Indexed keywords

CARBAZOLE DERIVATIVE; CD135 ANTIGEN; FLT3 PROTEIN, HUMAN; FLT3 PROTEIN, MOUSE; INDOLE DERIVATIVE; PROTEIN KINASE INHIBITOR; TTT-3002;

EID: 84907487835     PISSN: 00085472     EISSN: 15387445     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-14-1028     Document Type: Article
Times cited : (22)

References (41)
  • 1
    • 0030451722 scopus 로고    scopus 로고
    • Internal tandem duplication of the flt3 gene found in acute myeloid leukemia
    • Nakao M, Yokota S, Iwai T, Kaneko H, Horiike S, Kashima K, et al. Internal tandem duplication of the flt3 gene found in acute myeloid leukemia. Leukemia 1996;10:1911-8.
    • (1996) Leukemia , vol.10 , pp. 1911-1918
    • Nakao, M.1    Yokota, S.2    Iwai, T.3    Kaneko, H.4    Horiike, S.5    Kashima, K.6
  • 2
    • 0035871889 scopus 로고    scopus 로고
    • Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies
    • Yamamoto Y, Kiyoi H, Nakano Y, Suzuki R, Kodera Y, Miyawaki S, et al. Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies. Blood 2001;97:2434-9.
    • (2001) Blood , vol.97 , pp. 2434-2439
    • Yamamoto, Y.1    Kiyoi, H.2    Nakano, Y.3    Suzuki, R.4    Kodera, Y.5    Miyawaki, S.6
  • 3
  • 4
    • 1842420032 scopus 로고    scopus 로고
    • Singleagent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia
    • Smith BD, Levis M, Beran M, Giles F, Kantarjian H, Berg K, et al. Singleagent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia. Blood 2004;103:3669-76.
    • (2004) Blood , vol.103 , pp. 3669-3676
    • Smith, B.D.1    Levis, M.2    Beran, M.3    Giles, F.4    Kantarjian, H.5    Berg, K.6
  • 5
    • 79953124734 scopus 로고    scopus 로고
    • Results from a randomized trial of salvage chemotherapy followed by lestaurtinib for patients with FLT3 mutant AML in first relapse
    • Levis M, Ravandi F, Wang ES, Baer MR, Perl A, Coutre S, et al. Results from a randomized trial of salvage chemotherapy followed by lestaurtinib for patients with FLT3 mutant AML in first relapse. Blood 2011;117:3294-301.
    • (2011) Blood , vol.117 , pp. 3294-3301
    • Levis, M.1    Ravandi, F.2    Wang, E.S.3    Baer, M.R.4    Perl, A.5    Coutre, S.6
  • 6
    • 0034684075 scopus 로고    scopus 로고
    • Role of alpha1 acid glycoprotein in the in vivo resistance of human BCR-ABL (+) leukemic cells to the abl inhibitor STI571
    • Gambacorti-Passerini C, Barni R, le Coutre P, Zucchetti M, Cabrita G, Cleris L, et al. Role of alpha1 acid glycoprotein in the in vivo resistance of human BCR-ABL (+) leukemic cells to the abl inhibitor STI571. J Natl Cancer Inst 2000;92:1641-50.
    • (2000) J Natl Cancer Inst , vol.92 , pp. 1641-1650
    • Gambacorti-Passerini, C.1    Barni, R.2    Le Coutre, P.3    Zucchetti, M.4    Cabrita, G.5    Cleris, L.6
  • 7
    • 33751170444 scopus 로고    scopus 로고
    • Plasma inhibitory activity (PIA): A pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors
    • Levis M, Brown P, Smith BD, Stine A, Pham R, Stone R, et al. Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors. Blood 2006;108:3477-83.
    • (2006) Blood , vol.108 , pp. 3477-3483
    • Levis, M.1    Brown, P.2    Smith, B.D.3    Stine, A.4    Pham, R.5    Stone, R.6
  • 11
    • 77951645227 scopus 로고    scopus 로고
    • Phase I/II study of combination therapy with sorafenib, idarubicin, and cytarabine in younger patients with acute myeloid leukemia
    • Ravandi F, Cortes JE, Jones D, Faderl S, Garcia-Manero G, Konopleva MY, et al. Phase I/II study of combination therapy with sorafenib, idarubicin, and cytarabine in younger patients with acute myeloid leukemia. J Clin Oncol 2010;28:1856-62.
    • (2010) J Clin Oncol , vol.28 , pp. 1856-1862
    • Ravandi, F.1    Cortes, J.E.2    Jones, D.3    Faderl, S.4    Garcia-Manero, G.5    Konopleva, M.Y.6
  • 12
    • 80052231301 scopus 로고    scopus 로고
    • FLT3 inhibition as therapy in acute myeloid leukemia: A record of trials and tribulations
    • Fathi AT, Chabner BA. FLT3 inhibition as therapy in acute myeloid leukemia: a record of trials and tribulations. Oncologist 2011;16:1162-74.
    • (2011) Oncologist , vol.16 , pp. 1162-1174
    • Fathi, A.T.1    Chabner, B.A.2
  • 13
    • 78049426367 scopus 로고    scopus 로고
    • Phase IIB trial of oral midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3
    • Fischer T, Stone RM, Deangelo DJ, Galinsky I, Estey E, Lanza C, et al. Phase IIB trial of oral midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3. J Clin Oncol 2010;28:4339-45.
    • (2010) J Clin Oncol , vol.28 , pp. 4339-4345
    • Fischer, T.1    Stone, R.M.2    Deangelo, D.J.3    Galinsky, I.4    Estey, E.5    Lanza, C.6
  • 14
    • 39649097219 scopus 로고    scopus 로고
    • Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin
    • Barry EV, Clark JJ, Cools J, Roesel J, Gilliland DG. Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin. Blood 2007;110:4476-9.
    • (2007) Blood , vol.110 , pp. 4476-4479
    • Barry, E.V.1    Clark, J.J.2    Cools, J.3    Roesel, J.4    Gilliland, D.G.5
  • 15
    • 7244251613 scopus 로고    scopus 로고
    • Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518
    • Clark JJ, Cools J, Curley DP, Yu JC, Lokker NA, Giese NA, et al. Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518. Blood 2004;104:2867-72.
    • (2004) Blood , vol.104 , pp. 2867-2872
    • Clark, J.J.1    Cools, J.2    Curley, D.P.3    Yu, J.C.4    Lokker, N.A.5    Giese, N.A.6
  • 16
    • 34548691437 scopus 로고    scopus 로고
    • Sensitivity toward sorafenib and sunitinib varies between different activating and drugresistant FLT3-ITD mutations
    • Kancha RK, Grundler R, Peschel C, Duyster J. Sensitivity toward sorafenib and sunitinib varies between different activating and drugresistant FLT3-ITD mutations. Exp Hematol 2007;35:1522-6.
    • (2007) Exp Hematol , vol.35 , pp. 1522-1526
    • Kancha, R.K.1    Grundler, R.2    Peschel, C.3    Duyster, J.4
  • 17
    • 19944427559 scopus 로고    scopus 로고
    • Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412
    • Stone RM, DeAngelo DJ, Klimek V, Galinsky I, Estey E, Nimer SD, et al. Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412. Blood 2005;105:54-60.
    • (2005) Blood , vol.105 , pp. 54-60
    • Stone, R.M.1    DeAngelo, D.J.2    Klimek, V.3    Galinsky, I.4    Estey, E.5    Nimer, S.D.6
  • 18
    • 30144432781 scopus 로고    scopus 로고
    • Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of asn-676 in the FLT3 tyrosine kinase domain
    • Heidel F, Solem FK, Breitenbuecher F, Lipka DB, Kasper S, Thiede MH, et al. Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of asn-676 in the FLT3 tyrosine kinase domain. Blood 2006;107:293-300.
    • (2006) Blood , vol.107 , pp. 293-300
    • Heidel, F.1    Solem, F.K.2    Breitenbuecher, F.3    Lipka, D.B.4    Kasper, S.5    Thiede, M.H.6
  • 19
    • 84863785488 scopus 로고    scopus 로고
    • Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: A model for emerging clinical resistance patterns
    • Moore AS, Faisal A, Gonzalez de Castro D, Bavetsias V, Sun C, Atrash B, et al. Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. Leukemia 2012;26:1462-70.
    • (2012) Leukemia , vol.26 , pp. 1462-1470
    • Moore, A.S.1    Faisal, A.2    De Castro, G.D.3    Bavetsias, V.4    Sun, C.5    Atrash, B.6
  • 20
    • 84860747223 scopus 로고    scopus 로고
    • Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia
    • Smith CC, Wang Q, Chin CS, Salerno S, Damon LE, Levis MJ, et al. Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia. Nature 2012;485:260-3.
    • (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
  • 21
    • 84891814607 scopus 로고    scopus 로고
    • Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants
    • Galanis A, Ma H, Rajkhowa T, Ramachandran A, Small D, Cortes J, et al. Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants. Blood 2014;123:94-100.
    • (2014) Blood , vol.123 , pp. 94-100
    • Galanis, A.1    Ma, H.2    Rajkhowa, T.3    Ramachandran, A.4    Small, D.5    Cortes, J.6
  • 22
    • 84888263107 scopus 로고    scopus 로고
    • Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia
    • Zimmerman EI, Turner DC, Buaboonnam J, Hu S, Orwick S, Roberts MS, et al. Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia. Blood 2013;122:3607-15.
    • (2013) Blood , vol.122 , pp. 3607-3615
    • Zimmerman, E.I.1    Turner, D.C.2    Buaboonnam, J.3    Hu, S.4    Orwick, S.5    Roberts, M.S.6
  • 23
    • 84879165997 scopus 로고    scopus 로고
    • Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD
    • Smith CC, Lasater EA, Zhu X, Lin KC, Stewart WK, Damon LE, et al. Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD. Blood 2013;121:3165-71.
    • (2013) Blood , vol.121 , pp. 3165-3171
    • Smith, C.C.1    Lasater, E.A.2    Zhu, X.3    Lin, K.C.4    Stewart, W.K.5    Damon, L.E.6
  • 24
    • 84897557274 scopus 로고    scopus 로고
    • TTT-3002 is a novel FLT3 tyrosine kinase inhibitor with activity against FLT3-associated leukemias in vitro and in vivo
    • Ma H, Nguyen B, Li L, Greenblatt S, Williams A, Zhao M, et al. TTT-3002 is a novel FLT3 tyrosine kinase inhibitor with activity against FLT3-associated leukemias in vitro and in vivo. Blood 2014;123:1525-34.
    • (2014) Blood , vol.123 , pp. 1525-1534
    • Ma, H.1    Nguyen, B.2    Li, L.3    Greenblatt, S.4    Williams, A.5    Zhao, M.6
  • 25
    • 0842310394 scopus 로고    scopus 로고
    • The structural basis for autoinhibition of FLT3 by the juxtamembrane domain
    • Griffith J, Black J, Faerman C, Swenson L, Wynn M, Lu F, et al. The structural basis for autoinhibition of FLT3 by the juxtamembrane domain. Mol Cell 2004;13:169-78.
    • (2004) Mol Cell , vol.13 , pp. 169-178
    • Griffith, J.1    Black, J.2    Faerman, C.3    Swenson, L.4    Wynn, M.5    Lu, F.6
  • 26
    • 84867816311 scopus 로고    scopus 로고
    • Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors
    • McTigue M, Murray BW, Chen JH, Deng YL, Solowiej J, Kania RS. Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors. Proc Natl Acad Sci U S A 2012;109:18281-9.
    • (2012) Proc Natl Acad Sci U S A , vol.109 , pp. 18281-18289
    • McTigue, M.1    Murray, B.W.2    Chen, J.H.3    Deng, Y.L.4    Solowiej, J.5    Kania, R.S.6
  • 27
    • 0033555270 scopus 로고    scopus 로고
    • Structure of the protein tyrosine kinase domain of C-terminal src kinase (CSK) in complex with staurosporine
    • Lamers MB, Antson AA, Hubbard RE, Scott RK, Williams DH. Structure of the protein tyrosine kinase domain of C-terminal src kinase (CSK) in complex with staurosporine. J Mol Biol 1999;285:713-25.
    • (1999) J Mol Biol , vol.285 , pp. 713-725
    • Lamers, M.B.1    Antson, A.A.2    Hubbard, R.E.3    Scott, R.K.4    Williams, D.H.5
  • 29
    • 84873567125 scopus 로고    scopus 로고
    • Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors
    • Williams AB, Nguyen B, Li L, Brown P, Levis M, Leahy D, et al. Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors. Leukemia 2013;27:48-55.
    • (2013) Leukemia , vol.27 , pp. 48-55
    • Williams, A.B.1    Nguyen, B.2    Li, L.3    Brown, P.4    Levis, M.5    Leahy, D.6
  • 30
    • 79953115783 scopus 로고    scopus 로고
    • Defective nonhomologous end joining blocks B-cell development in FLT3/ITD mice
    • Li L, Zhang L, Fan J, Greenberg K, Desiderio S, Rassool FV, et al. Defective nonhomologous end joining blocks B-cell development in FLT3/ITD mice. Blood 2011;117:3131-9.
    • (2011) Blood , vol.117 , pp. 3131-3139
    • Li, L.1    Zhang, L.2    Fan, J.3    Greenberg, K.4    Desiderio, S.5    Rassool, F.V.6
  • 31
    • 0037097716 scopus 로고    scopus 로고
    • Analysis of FLT3-activating mutations in 979 patients with acute myelogenous leukemia: Association with FAB subtypes and identification of subgroups with poor prognosis
    • Thiede C, Steudel C, Mohr B, Schaich M, Schakel U, Platzbecker U, et al. Analysis of FLT3-activating mutations in 979 patients with acute myelogenous leukemia: association with FAB subtypes and identification of subgroups with poor prognosis. Blood 2002;99:4326-35.
    • (2002) Blood , vol.99 , pp. 4326-4335
    • Thiede, C.1    Steudel, C.2    Mohr, B.3    Schaich, M.4    Schakel, U.5    Platzbecker, U.6
  • 33
    • 0037114829 scopus 로고    scopus 로고
    • Prognostic significance of activating FLT3 mutations in younger adults (16 to 60 years) with acute myeloid leukemia and normal cytogenetics: A study of the AML study group ulm
    • Frohling S, Schlenk RF, Breitruck J, Benner A, Kreitmeier S, Tobis K, et al. Prognostic significance of activating FLT3 mutations in younger adults (16 to 60 years) with acute myeloid leukemia and normal cytogenetics: a study of the AML study group ulm. Blood 2002;100:4372-80.
    • (2002) Blood , vol.100 , pp. 4372-4380
    • Frohling, S.1    Schlenk, R.F.2    Breitruck, J.3    Benner, A.4    Kreitmeier, S.5    Tobis, K.6
  • 35
    • 84861906112 scopus 로고    scopus 로고
    • Sorafenib treatment of FLT3-ITD (+) acute myeloid leukemia: Favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation
    • Man CH, Fung TK, Ho C, Han HH, Chow HC, Ma AC, et al. Sorafenib treatment of FLT3-ITD (+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation. Blood 2012;119:5133-43.
    • (2012) Blood , vol.119 , pp. 5133-5143
    • Man, C.H.1    Fung, T.K.2    Ho, C.3    Han, H.H.4    Chow, H.C.5    Ma, A.C.6
  • 36
    • 84873083526 scopus 로고    scopus 로고
    • FLT3 inhibitor treatment in FLT3-mutated AML is associated with development of secondary FLT3-TKD mutations
    • Alvarado T, Kantarjian H, Ravandi F, Luthra R, Borthakur G, Manero GG, et al. FLT3 inhibitor treatment in FLT3-mutated AML is associated with development of secondary FLT3-TKD mutations. Blood 2008;118:1493.
    • (2008) Blood , vol.118 , pp. 1493
    • Alvarado, T.1    Kantarjian, H.2    Ravandi, F.3    Luthra, R.4    Borthakur, G.5    Manero, G.G.6
  • 37
    • 84873078929 scopus 로고    scopus 로고
    • Acquired point mutations of TKD are responsible for sorafenib resistance in FLT3-ITD mutant AML
    • Zhang W, Konopleva M, Jacamo RO, Borthakur G, Chen W, Cortes J, et al. Acquired point mutations of TKD are responsible for sorafenib resistance in FLT3-ITD mutant AML. Blood 2011;118.
    • (2011) Blood , pp. 118
    • Zhang, W.1    Konopleva, M.2    Jacamo, R.O.3    Borthakur, G.4    Chen, W.5    Cortes, J.6
  • 38
    • 4644240387 scopus 로고    scopus 로고
    • Prediction of resistance to small molecule FLT3 inhibitors: Implications for molecularly targeted therapy of acute leukemia
    • Cools J, Mentens N, Furet P, Fabbro D, Clark JJ, Griffin JD, et al. Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia. Cancer Res 2004;64:6385-9.
    • (2004) Cancer Res , vol.64 , pp. 6385-6389
    • Cools, J.1    Mentens, N.2    Furet, P.3    Fabbro, D.4    Clark, J.J.5    Griffin, J.D.6
  • 39
    • 84875492999 scopus 로고    scopus 로고
    • Plasma protein binding of sorafenib, a multi kinase inhibitor: In vitro and in cancer patients
    • Villarroel MC, Pratz KW, Xu L, Wright JJ, Smith BD, Rudek MA. Plasma protein binding of sorafenib, a multi kinase inhibitor: in vitro and in cancer patients. Invest New Drugs 2012;30:2096-102.
    • (2012) Invest New Drugs , vol.30 , pp. 2096-2102
    • Villarroel, M.C.1    Pratz, K.W.2    Xu, L.3    Wright, J.J.4    Smith, B.D.5    Rudek, M.A.6
  • 40
    • 0023690101 scopus 로고
    • Drug binding to human alpha-1-acid glycoprotein in health and disease
    • Kremer JM, Wilting J, Janssen LH. Drug binding to human alpha-1-acid glycoprotein in health and disease. Pharmacol Rev 1988;40:1-47.
    • (1988) Pharmacol Rev , vol.40 , pp. 1-47
    • Kremer, J.M.1    Wilting, J.2    Janssen, L.H.3
  • 41
    • 70449475105 scopus 로고    scopus 로고
    • AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)
    • Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 2009;114:2984-92.
    • (2009) Blood , vol.114 , pp. 2984-2992
    • Zarrinkar, P.P.1    Gunawardane, R.N.2    Cramer, M.D.3    Gardner, M.F.4    Brigham, D.5    Belli, B.6


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