메뉴 건너뛰기




Volumn 144, Issue 6, 2009, Pages 865-874

Bis(1H-indol-2-yl)methanones are effective inhibitors of FLT3-ITD tyrosine kinase and partially overcome resistance to PKC412A in vitro

Author keywords

Acute myeloid leukaemia; Fms like tyrosine kinase 3; Resistance; Small molecule; Tyrosine kinase inhibitor

Indexed keywords

BIS(1H INDOL 2 YL)METHANONE DERIVATIVE; CD135 ANTIGEN; CYTARABINE; DAUNORUBICIN; MIDOSTAURIN; MITOGEN ACTIVATED PROTEIN KINASE; PROTEIN KINASE B; PROTEIN TYROSINE KINASE INHIBITOR; STAT5 PROTEIN; UNCLASSIFIED DRUG;

EID: 60749136351     PISSN: 00071048     EISSN: 13652141     Source Type: Journal    
DOI: 10.1111/j.1365-2141.2008.07567.x     Document Type: Article
Times cited : (10)

References (33)
  • 2
    • 84868893925 scopus 로고    scopus 로고
    • The FLT3 inhibitor PKC412 displays a limited set of specific FLT3-ITD resistance mutations which in a cell-based screen is not overlapping with the su5614 resistance profile
    • abstract P449).
    • von Bubnoff, N., Sänger, J., Peschel, C. Duyster, J. (2007 The FLT3 inhibitor PKC412 displays a limited set of specific FLT3-ITD resistance mutations which in a cell-based screen is not overlapping with the su5614 resistance profile. Onkologie, 30, 108 (abstract P449).
    • (2007) Onkologie , vol.30 , pp. 108
    • Von Bubnoff, N.1    Sänger, J.2    Peschel, C.3    Duyster, J.4
  • 3
    • 33748794547 scopus 로고    scopus 로고
    • Theoretical basis, experimental design, and computerized simulation of synergism and antagonism in drug combination studies
    • Chou, T.C. (2006) Theoretical basis, experimental design, and computerized simulation of synergism and antagonism in drug combination studies. Pharmacological Reviews, 58, 621 681.
    • (2006) Pharmacological Reviews , vol.58 , pp. 621-681
    • Chou, T.C.1
  • 4
    • 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, J.J., Griffin, J.D., Marynen, P. Gilliland, D.G. (2004) Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia. Cancer Research, 64, 6385 6389.
    • (2004) Cancer Research , 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    Marynen, P.7    Gilliland, D.G.8
  • 6
    • 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, R.F., Breitruck, J., Benner, A., Kreitmeier, S., Tobis, K., Dohner, H. Dohner, K. (2002) 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, 100, 4372 4380.
    • (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    Dohner, H.7    Dohner, K.8
  • 7
    • 33746716196 scopus 로고    scopus 로고
    • Aromatic interactions with phenylalanine 691 and cysteine 828: A concept for FMS-like tyrosine kinase-3 inhibition. Application to the discovery of a new class of potential antileukemia agents
    • Furet, P., Bold, G., Meyer, T., Roesel, J. Guagnano, V. (2006) Aromatic interactions with phenylalanine 691 and cysteine 828: a concept for FMS-like tyrosine kinase-3 inhibition. Application to the discovery of a new class of potential antileukemia agents. Journal of Medicinal Chemistry, 49, 4451 4454.
    • (2006) Journal of Medicinal Chemistry , vol.49 , pp. 4451-4454
    • Furet, P.1    Bold, G.2    Meyer, T.3    Roesel, J.4    Guagnano, V.5
  • 8
    • 0035469856 scopus 로고    scopus 로고
    • Attempts to improve treatment outcomes in acute myeloid leukemia (AML) in older patients: The results of the United Kingdom Medical Research Council AML11 trial
    • Goldstone, A.H., Burnett, A.K., Wheatley, K., Smith, A.G., Hutchinson, R.M. Clark, R.E. (2001) Attempts to improve treatment outcomes in acute myeloid leukemia (AML) in older patients: the results of the United Kingdom Medical Research Council AML11 trial. Blood, 98, 1302 1311.
    • (2001) Blood , vol.98 , pp. 1302-1311
    • Goldstone, A.H.1    Burnett, A.K.2    Wheatley, K.3    Smith, A.G.4    Hutchinson, R.M.5    Clark, R.E.6
  • 9
    • 33947596047 scopus 로고    scopus 로고
    • A neoepitope generated by an FLT3 internal tandem duplication (FLT3-ITD) is recognized by leukemia-reactive autologous CD8+ T cells
    • Graf, C., Heidel, F., Tenzer, S., Radsak, M.P., Solem, F.K., Britten, C.M., Huber, C., Fischer, T. Wolfel, T. (2007) A neoepitope generated by an FLT3 internal tandem duplication (FLT3-ITD) is recognized by leukemia-reactive autologous CD8+ T cells. Blood, 109, 2985 2988.
    • (2007) Blood , vol.109 , pp. 2985-2988
    • Graf, C.1    Heidel, F.2    Tenzer, S.3    Radsak, M.P.4    Solem, F.K.5    Britten, C.M.6    Huber, C.7    Fischer, T.8    Wolfel, T.9
  • 12
    • 34548691437 scopus 로고    scopus 로고
    • Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations
    • Kancha, R.K., Grundler, R., Peschel, C. Duyster, J. (2007) Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations. Experimental Hematology, 35, 1522 1526.
    • (2007) Experimental Hematology , vol.35 , pp. 1522-1526
    • Kancha, R.K.1    Grundler, R.2    Peschel, C.3    Duyster, J.4
  • 13
    • 0036093475 scopus 로고    scopus 로고
    • FLT3 internal tandem duplication mutations associated with human acute myeloid leukemias induce myeloproliferative disease in a murine bone marrow transplant model
    • Kelly, L.M., Liu, Q., Kutok, J.L., Williams, I.R., Boulton, C.L. Gilliland, D.G. (2002) FLT3 internal tandem duplication mutations associated with human acute myeloid leukemias induce myeloproliferative disease in a murine bone marrow transplant model. Blood, 99, 310 318.
    • (2002) Blood , vol.99 , pp. 310-318
    • Kelly, L.M.1    Liu, Q.2    Kutok, J.L.3    Williams, I.R.4    Boulton, C.L.5    Gilliland, D.G.6
  • 14
    • 0038040669 scopus 로고    scopus 로고
    • In BCR-ABL-positive cells, STAT-5 tyrosine-phosphorylation integrates signals induced by imatinib mesylate and Ara-C
    • Kindler, T., Breitenbuecher, F., Kasper, S., Stevens, T., Carius, B., Gschaidmeier, H., Huber, C. Fischer, T. (2003) In BCR-ABL-positive cells, STAT-5 tyrosine-phosphorylation integrates signals induced by imatinib mesylate and Ara-C. Leukemia, 17, 999 1009.
    • (2003) Leukemia , vol.17 , pp. 999-1009
    • Kindler, T.1    Breitenbuecher, F.2    Kasper, S.3    Stevens, T.4    Carius, B.5    Gschaidmeier, H.6    Huber, C.7    Fischer, T.8
  • 17
    • 33751173636 scopus 로고    scopus 로고
    • A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy
    • Knapper, S., Burnett, A.K., Littlewood, T., Kell, W.J., Agrawal, S., Chopra, R., Clark, R., Levis, M.J. Small, D. (2006) A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy. Blood, 108, 3262 3270.
    • (2006) Blood , vol.108 , pp. 3262-3270
    • Knapper, S.1    Burnett, A.K.2    Littlewood, T.3    Kell, W.J.4    Agrawal, S.5    Chopra, R.6    Clark, R.7    Levis, M.J.8    Small, D.9
  • 18
    • 0343045296 scopus 로고    scopus 로고
    • Mitoxantrone versus daunorubicin in induction-consolidation chemotherapy - The value of low-dose cytarabine for maintenance of remission, and an assessment of prognostic factors in acute myeloid leukemia in the elderly: Final report. European Organization for the Research and Treatment of Cancer and the Dutch-Belgian Hemato-Oncology Cooperative Hovon Group
    • Lowenberg, B., Suciu, S., Archimbaud, E., Haak, H., Stryckmans, P., de Cataldo, R., Dekker, A.W., Berneman, Z.N., Thyss, A., van der Lelie, J., Sonneveld, P., Visani, G., Fillet, G., Hayat, M., Hagemeijer, A., Solbu, G. Zittoun, R. (1998) Mitoxantrone versus daunorubicin in induction-consolidation chemotherapy - the value of low-dose cytarabine for maintenance of remission, and an assessment of prognostic factors in acute myeloid leukemia in the elderly: final report. European Organization for the Research and Treatment of Cancer and the Dutch-Belgian Hemato-Oncology Cooperative Hovon Group. Journal of Clinical Oncology, 16, 872 881.
    • (1998) Journal of Clinical Oncology , vol.16 , pp. 872-881
    • Lowenberg, B.1    Suciu, S.2    Archimbaud, E.3    Haak, H.4    Stryckmans, P.5    De Cataldo, R.6    Dekker, A.W.7    Berneman, Z.N.8    Thyss, A.9    Van Der Lelie, J.10    Sonneveld, P.11    Visani, G.12    Fillet, G.13    Hayat, M.14    Hagemeijer, A.15    Solbu, G.16    Zittoun, R.17
  • 23
  • 24
    • 34548825795 scopus 로고    scopus 로고
    • Bcr-Abl kinase domain mutations, drug resistance, and the road to a cure for chronic myeloid leukemia
    • O'Hare, T., Eide, C.A. Deininger, M.W. (2007) Bcr-Abl kinase domain mutations, drug resistance, and the road to a cure for chronic myeloid leukemia. Blood, 110, 2242 2249.
    • (2007) Blood , vol.110 , pp. 2242-2249
    • O'Hare, T.1    Eide, C.A.2    Deininger, M.W.3
  • 25
    • 33646432479 scopus 로고    scopus 로고
    • IMC-EB10, an anti-FLT3 monoclonal antibody, prolongs survival and reduces nonobese diabetic/severe combined immunodeficient engraftment of some acute lymphoblastic leukemia cell lines and primary leukemic samples
    • Piloto, O., Nguyen, B., Huso, D., Kim, K.T., Li, Y., Witte, L., Hicklin, D.J., Brown, P. Small, D. (2006) IMC-EB10, an anti-FLT3 monoclonal antibody, prolongs survival and reduces nonobese diabetic/severe combined immunodeficient engraftment of some acute lymphoblastic leukemia cell lines and primary leukemic samples. Cancer Research, 66, 4843 4851.
    • (2006) Cancer Research , vol.66 , pp. 4843-4851
    • Piloto, O.1    Nguyen, B.2    Huso, D.3    Kim, K.T.4    Li, Y.5    Witte, L.6    Hicklin, D.J.7    Brown, P.8    Small, D.9
  • 26
    • 33846936758 scopus 로고    scopus 로고
    • Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathways
    • Piloto, O., Wright, M., Brown, P., Kim, K.T., Levis, M. Small, D. (2007) Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathways. Blood, 109, 1643 1652.
    • (2007) Blood , vol.109 , pp. 1643-1652
    • Piloto, O.1    Wright, M.2    Brown, P.3    Kim, K.T.4    Levis, M.5    Small, D.6
  • 28
  • 30
    • 34249829699 scopus 로고    scopus 로고
    • Phase IB study of PKC412, an oral FLT3 kinase inhibitor, in sequential and simultaneous combinations with daunorubicin and cytarabine (DA) induction and high-dose cytarabine consolidation in newly diagnosed adult patients (pts) with acute myeloid leukemia (AML) under age 61
    • Stone, R.M., Fischer, T., Paquette, R., Schiller, G., Schiffer, C.A., Ehninger, G., Cortes, J., Kantarjian, H., DeAngelo, D.A., Massimini, G., Li, X., Phillips, P. Giles, F. (2006) Phase IB study of PKC412, an oral FLT3 kinase inhibitor, in sequential and simultaneous combinations with daunorubicin and cytarabine (DA) induction and high-dose cytarabine consolidation in newly diagnosed adult patients (pts) with acute myeloid leukemia (AML) under age 61. Blood (ASH Annual Meeting Abstracts), 108, 157.
    • (2006) Blood (ASH Annual Meeting Abstracts) , vol.108 , pp. 157
    • Stone, R.M.1    Fischer, T.2    Paquette, R.3    Schiller, G.4    Schiffer, C.A.5    Ehninger, G.6    Cortes, J.7    Kantarjian, H.8    Deangelo, D.A.9    Massimini, G.10    Li, X.11    Phillips, P.12    Giles, F.13
  • 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., Wermke, M., Bornhauser, M., Ritter, M., Neubauer, A., Ehninger, G. Illmer, T. (2002) Analysis of FLT3-activating mutations in 979 patients with acute myelogenous leukemia: association with FAB subtypes and identification of subgroups with poor prognosis. Blood, 99, 4326 4335.
    • (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    Wermke, M.7    Bornhauser, M.8    Ritter, M.9    Neubauer, A.10    Ehninger, G.11    Illmer, T.12
  • 33
    • 16944365287 scopus 로고    scopus 로고
    • Internal tandem duplication of the FLT3 gene is preferentially seen in acute myeloid leukemia and myelodysplastic syndrome among various hematological malignancies. A study on a large series of patients and cell lines
    • Yokota, S., Kiyoi, H., Nakao, M., Iwai, T., Misawa, S., Okuda, T., Sonoda, Y., Abe, T., Kahsima, K., Matsuo, Y. Naoe, T. (1997) Internal tandem duplication of the FLT3 gene is preferentially seen in acute myeloid leukemia and myelodysplastic syndrome among various hematological malignancies. A study on a large series of patients and cell lines. Leukemia, 11, 1605 1609.
    • (1997) Leukemia , vol.11 , pp. 1605-1609
    • Yokota, S.1    Kiyoi, H.2    Nakao, M.3    Iwai, T.4    Misawa, S.5    Okuda, T.6    Sonoda, Y.7    Abe, T.8    Kahsima, K.9    Matsuo, Y.10    Naoe, T.11


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.