The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib

被引：50
作者：
Albers, C. [1 ]
Leischner, H. [1 ]
Verbeek, M. [1 ]
Yu, C. [1 ]
Illert, A. L. [2 ]
Peschel, C. [1 ]
von Bubnoff, N. [2 ]
Duyster, J. [2 ]
机构：
[1] Tech Univ Munich, Klinikum Rechts Isar, Dept Internal Med 3, D-80290 Munich, Germany
[2] Univ Med Ctr Freiburg, Dept Hematol Oncol, Freiburg, Germany
来源：
LEUKEMIA | 2013年 / 27卷 / 06期
关键词：
ACUTE MYELOID-LEUKEMIA; CLINICAL RESISTANCE; INHIBITORS; SORAFENIB;
D O I：
10.1038/leu.2013.14
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
引用
收藏
页码：1416 / 1418
页数：4
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共 8 条
  • [1] 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
    Marynen, P
    Gilliland, DG
    [J]. CANCER RESEARCH, 2004, 64 (18) : 6385 - 6389
  • [2] 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
    Brandts, C
    Serve, H
    Roesel, J
    Giles, F
    Feldman, E
    Ehninger, G
    Schiller, GJ
    Nimer, S
    Stone, RM
    Wang, YF
    Kindler, T
    Cohen, PS
    Huber, C
    Fischer, T
    [J]. BLOOD, 2006, 107 (01) : 293 - 300
  • [3] Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations
    Kancha, Rama Krishna
    Grundler, Rebekka
    Peschel, Christian
    Duyster, Justus
    [J]. EXPERIMENTAL HEMATOLOGY, 2007, 35 (10) : 1522 - 1526
  • [4] Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns
    Moore, A. S.
    Faisal, A.
    de Castro, D. Gonzalez
    Bavetsias, V.
    Sun, C.
    Atrash, B.
    Valenti, M.
    Brandon, A. de Haven
    Avery, S.
    Mair, D.
    Mirabella, F.
    Swansbury, J.
    Pearson, A. D. J.
    Workman, P.
    Blagg, J.
    Raynaud, F. I.
    Eccles, S. A.
    Linardopoulos, S.
    [J]. LEUKEMIA, 2012, 26 (07) : 1462 - 1470
  • [5] Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia
    Smith, Catherine C.
    Wang, Qi
    Chin, Chen-Shan
    Salerno, Sara
    Damon, Lauren E.
    Levis, Mark J.
    Perl, Alexander E.
    Travers, Kevin J.
    Wang, Susana
    Hunt, Jeremy P.
    Zarrinkar, Patrick P.
    Schadt, Eric E.
    Kasarskis, Andrew
    Kuriyan, John
    Shah, Neil P.
    [J]. NATURE, 2012, 485 (7397) : 260 - U153
  • [6] Identification of a secondary FLT3/A848P mutation in a patient with FLT3-ITD-positive blast phase CMML and response to sunitinib and sorafenib
    von Bubnoff, N.
    Rummelt, C.
    Menzel, H.
    Sigl, M.
    Peschel, C.
    Duyster, J.
    [J]. LEUKEMIA, 2010, 24 (08) : 1523 - 1525
  • [7] FMS-Like Tyrosine Kinase 3-Internal Tandem Duplication Tyrosine Kinase Inhibitors Display a Nonoverlapping Profile of Resistance Mutations In vitro
    von Bubnoff, Nikolas
    Engh, Richard A.
    Aberg, Espen
    Sanger, Jana
    Peschel, Christian
    Duyster, Justus
    [J]. CANCER RESEARCH, 2009, 69 (07) : 3032 - 3041
  • [8] AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)
    Zarrinkar, Patrick P.
    Gunawardane, Ruwanthi N.
    Cramer, Merryl D.
    Gardner, Michael F.
    Brigham, Daniel
    Belli, Barbara
    Karaman, Mazen W.
    Pratz, Keith W.
    Pallares, Gabriel
    Chao, Qi
    Sprankle, Kelly G.
    Patel, Hitesh K.
    Levis, Mark
    Armstrong, Robert C.
    James, Joyce
    Bhagwat, Shripad S.
    [J]. BLOOD, 2009, 114 (14) : 2984 - 2992
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