Drug resistance in mutant FLT3-positive AML.

scientific article published on 12 July 2010

Drug resistance in mutant FLT3-positive AML. is …
instance of (P31):
review articleQ7318358
scholarly articleQ13442814

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P6179Dimensions Publication ID1047102240
P356DOI10.1038/ONC.2010.273
P698PubMed publication ID20622902
P5875ResearchGate publication ID45151862

P2093author name stringM Sattler
J D Griffin
A Ray
E Weisberg
P2860cites workThe role of FLT3 in haematopoietic malignanciesQ24319174
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Inhibition of the transforming activity of FLT3 internal tandem duplication mutants from AML patients by a tyrosine kinase inhibitorQ27824787
A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndromeQ27824793
Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemiaQ27824808
FLT3-ITD-TKD dual mutants associated with AML confer resistance to FLT3 PTK inhibitors and cytotoxic agents by overexpression of Bcl-x(L).Q27824823
Mutant FLT3: a direct target of sorafenib in acute myelogenous leukemiaQ27851423
FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitroQ27851469
Smac, a mitochondrial protein that promotes cytochrome c-dependent caspase activation by eliminating IAP inhibitionQ28115131
A FLT3-targeted tyrosine kinase inhibitor is cytotoxic to leukemia cells in vitro and in vivoQ28217482
Compassionate use of sorafenib in FLT3-ITD-positive acute myeloid leukemia: sustained regression before and after allogeneic stem cell transplantationQ28242368
Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemiaQ29615030
Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplificationQ29618788
Overriding imatinib resistance with a novel ABL kinase inhibitorQ30014844
Bis(1H-2-indolyl)-1-methanones as inhibitors of the hematopoietic tyrosine kinase Flt3.Q40714821
FLT3 internal tandem duplication mutations associated with human acute myeloid leukemias induce myeloproliferative disease in a murine bone marrow transplant modelQ40760923
Inhibition of FLT3-mediated transformation by use of a tyrosine kinase inhibitorQ40792187
Cell differentiation in acute myeloid leukemia.Q41027015
The splenic microenvironment is a source of proangiogenesis/inflammatory mediators accelerating the expansion of murine erythroleukemic cellsQ42015052
A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical responseQ42192063
Simultaneous activation of multiple signal transduction pathways confers poor prognosis in acute myelogenous leukemiaQ42742064
Gain-of-function of mutated C-CBL tumour suppressor in myeloid neoplasmsQ42795736
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.Q42815284
250K single nucleotide polymorphism array karyotyping identifies acquired uniparental disomy and homozygous mutations, including novel missense substitutions of c-Cbl, in myeloid malignanciesQ43078973
Dual treatment with FLT3 inhibitor SU11657 and doxorubicin increases survival of leukemic miceQ43129559
CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML).Q44068434
Stromal cells prevent apoptosis of AML cells by up-regulation of anti-apoptotic proteinsQ44117862
SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinaseQ44155418
SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivoQ44280921
SU5416, a small molecule tyrosine kinase receptor inhibitor, has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromesQ44370169
Activating mutations of RTK/ras signal transduction pathway in pediatric acute myeloid leukemiaQ44408358
Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3).Q44483347
FLT3 internal tandem duplication in 234 children with acute myeloid leukemia: prognostic significance and relation to cellular drug resistanceQ44484460
FLT3 receptors with internal tandem duplications promote cell viability and proliferation by signaling through Foxo proteinsQ44775125
Effects of SU5416, a small molecule tyrosine kinase receptor inhibitor, on FLT3 expression and phosphorylation in patients with refractory acute myeloid leukemiaQ44906435
Identifying and characterizing a novel activating mutation of the FLT3 tyrosine kinase in AML.Q44922362
Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412.Q45042550
The expression of P-glycoprotein in AML cells with FLT3 internal tandem duplications is associated with reduced apoptosis in response to FLT3 inhibitorsQ45072250
Antileukemic activity of rapamycin in acute myeloid leukemia.Q45154681
Insertion of FLT3 internal tandem duplication in the tyrosine kinase domain-1 is associated with resistance to chemotherapy and inferior outcome.Q45929224
KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation.Q45960933
Identification of Ki23819, a highly potent inhibitor of kinase activity of mutant FLT3 receptor tyrosine kinaseQ46426194
The kinase inhibitor LS104 induces apoptosis, enhances cytotoxic effects of chemotherapeutic drugs and is targeting the receptor tyrosine kinase FLT3 in acute myeloid leukemiaQ46538314
CHIR-258: a potent inhibitor of FLT3 kinase in experimental tumor xenograft models of human acute myelogenous leukemiaQ46610628
Serum FLT-3 ligand in a busulphan-induced model of chronic bone marrow hypoplasia in the female CD-1 mouseQ46705750
Combined Abl inhibitor therapy for minimizing drug resistance in chronic myeloid leukemia: Src/Abl inhibitors are compatible with imatinibQ46735050
Constitutive activation of Akt by Flt3 internal tandem duplications is necessary for increased survival, proliferation, and myeloid transformation.Q46788369
In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptorQ46832743
Blockade of MEK/ERK signaling enhances sunitinib-induced growth inhibition and apoptosis of leukemia cells possessing activating mutations of the FLT3 geneQ46913925
The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia.Q46932190
Pediatric AML primary samples with FLT3/ITD mutations are preferentially killed by FLT3 inhibitionQ47422865
FLT3 and MLL intragenic abnormalities in AML reflect a common category of genotoxic stressQ47854939
Frequent CBL mutations associated with 11q acquired uniparental disomy in myeloproliferative neoplasmsQ47960630
Inhibition of CXCR4 with the novel RCP168 peptide overcomes stroma-mediated chemoresistance in chronic and acute leukemias.Q52575669
Targeting PIM kinases impairs survival of hematopoietic cells transformed by kinase inhibitor-sensitive and kinase inhibitor-resistant forms of Fms-like tyrosine kinase 3 and BCR/ABL.Q53347745
Adhesion to bone marrow stroma inhibits apoptosis of chronic lymphocytic leukemia cells.Q54067576
Flt3-dependent transformation by inactivating c-Cbl mutations in AMLQ57269958
A phase 2 clinical study of SU5416 in patients with refractory acute myeloid leukemiaQ58414438
Human bone marrow stromal cell contact and soluble factors have different effects on the survival and proliferation of paediatric B-lineage acute lymphoblastic leukaemic blastsQ72419337
Prognostic value of internal tandem duplication of the FLT3 gene in childhood acute myelogenous leukemiaQ73208706
Biological characteristics and prognosis of adult acute myeloid leukemia with internal tandem duplications in the Flt3 geneQ73674699
Tandem duplications of the FLT3 receptor gene are associated with leukemic transformation of myelodysplasiaQ73717211
Bone marrow stroma inhibits proliferation and apoptosis in leukemic cells through gap junction-mediated cell communicationQ73839468
Internal tandem duplication of the FLT3 gene is a novel modality of elongation mutation which causes constitutive activation of the productQ77299298
Endogenous FLT-3 ligand serum levels are associated with disease stage in patients with myelodysplastic syndromesQ77360733
Inhibition of Flt3-activating mutations does not prevent constitutive activation of ERK/Akt/STAT pathways in some AML cells: a possible cause for the limited effectiveness of monotherapy with small-molecule inhibitorsQ79384089
Bcr-Abl resistance screening predicts a limited spectrum of point mutations to be associated with clinical resistance to the Abl kinase inhibitor nilotinib (AMN107)Q83154106
Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis studyQ30158055
An efficient rapid system for profiling the cellular activities of molecular libraries.Q33234459
Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitorQ33241590
Antitumor activity of sorafenib in FLT3-driven leukemic cellsQ33268279
Novel and orally active 5-(1,3,4-oxadiazol-2-yl)pyrimidine derivatives as selective FLT3 inhibitorsQ33373888
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.Q33390054
Dissection of PIM serine/threonine kinases in FLT3-ITD-induced leukemogenesis reveals PIM1 as regulator of CXCL12-CXCR4-mediated homing and migrationQ33494281
XIAP is not required for human tumor cell survival in the absence of an exogenous death signalQ33523404
Altered thymic positive selection and intracellular signals in Cbl-deficient miceQ33596728
FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML.Q33680292
Mll rearrangements in haematological malignancies: lessons from clinical and biological studiesQ33723613
Tissue hyperplasia and enhanced T-cell signalling via ZAP-70 in c-Cbl-deficient miceQ33776192
Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistanceQ33927591
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412.Q34139532
Dasatinib inhibits the growth of molecularly heterogeneous myeloid leukemiasQ34335004
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 chemotherapyQ34549807
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dQ34573116
Mutations of e3 ubiquitin ligase cbl family members constitute a novel common pathogenic lesion in myeloid malignancies.Q34578265
Incorporating FLT3 inhibitors into acute myeloid leukemia treatment regimensQ34591403
Heat shock protein 90 inhibition is cytotoxic to primary AML cells expressing mutant FLT3 and results in altered downstream signalling.Q34765294
The roles of FLT3 in hematopoiesis and leukemiaQ34784925
Origins of chromosome translocations in childhood leukaemiaQ35210004
ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemiaQ35751114
Clinical implications of FLT3 mutations in pediatric AML.Q35848876
FLT3 internal tandem duplication in CD34+/CD33- precursors predicts poor outcome in acute myeloid leukemiaQ35849209
Roles of tyrosine 589 and 591 in STAT5 activation and transformation mediated by FLT3-ITD.Q35849949
Novel c-CBL and CBL-b ubiquitin ligase mutations in human acute myeloid leukemiaQ35901705
Highly phosphorylated FOXO3A is an adverse prognostic factor in acute myeloid leukemiaQ36065874
Negative regulation of PTK signalling by Cbl proteinsQ36194521
Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin.Q36447942
Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cellsQ36508937
The Jak2V617F oncogene associated with myeloproliferative diseases requires a functional FERM domain for transformation and for expression of the Myc and Pim proto-oncogenesQ36508949
Structural and numerical variation of FLT3/ITD in pediatric AML.Q36657987
Combination of rapamycin and protein tyrosine kinase (PTK) inhibitors for the treatment of leukemias caused by oncogenic PTKsQ36854122
BCR/ABL and other kinases from chronic myeloproliferative disorders stimulate single-strand annealing, an unfaithful DNA double-strand break repairQ36865331
Low frequency and variability of FLT3 mutations in Korean patients with acute myeloid leukemiaQ36966067
Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cellsQ37003553
Cytoprotective effects of IAPs revealed by a small molecule antagonistQ37172657
Cell cycle regulation by oncogenic tyrosine kinases in myeloid neoplasias: from molecular redox mechanisms to health implicationsQ37204275
Targeting the leukemia microenvironment by CXCR4 inhibition overcomes resistance to kinase inhibitors and chemotherapy in AML.Q37234641
BCR-ABL promotes the frequency of mutagenic single-strand annealing DNA repairQ37334605
Mutations in CBL occur frequently in juvenile myelomonocytic leukemiaQ37334614
Stroma-supported culture in childhood B-lineage acute lymphoblastic leukemia cells predicts treatment outcomeQ37351733
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)Q37373040
Mechanisms of resistance to FLT3 inhibitors.Q37375423
FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML.Q37495206
AML1-ETO downregulates the granulocytic differentiation factor C/EBPalpha in t(8;21) myeloid leukemia.Q38302335
A phase 1 study of SU11248 in the treatment of patients with refractory or resistant acute myeloid leukemia (AML) or not amenable to conventional therapy for the diseaseQ39218023
Mechanisms of resistance against PKC412 in resistant FLT3-ITD positive human acute myeloid leukemia cellsQ39745611
FLT3-ITD induces ara-C resistance in myeloid leukemic cells through the repression of the ENT1 expressionQ39784014
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitorQ39799665
CBL exon 8/9 mutants activate the FLT3 pathway and cluster in core binding factor/11q deletion acute myeloid leukemia/myelodysplastic syndrome subtypes.Q39874787
A novel molecular mechanism of primary resistance to FLT3-kinase inhibitors in AML.Q39895136
Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML.Q39895141
Targeting FMS-related tyrosine kinase receptor 3 with the human immunoglobulin G1 monoclonal antibody IMC-EB10.Q39904021
Stromal-mediated protection of tyrosine kinase inhibitor-treated BCR-ABL-expressing leukemia cellsQ39960316
Inhibition of apoptosome formation by suppression of Hsp90beta phosphorylation in tyrosine kinase-induced leukemiasQ39966770
Resistance to FLT3 inhibition in an in vitro model of primary AML cells with a stem cell phenotype in a defined microenvironment.Q39977455
Internal tandem duplication of FLT3 (FLT3/ITD) induces increased ROS production, DNA damage, and misrepair: implications for poor prognosis in AML.Q40025562
Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutationsQ40077336
A novel FLT3 inhibitor FI-700 selectively suppresses the growth of leukemia cells with FLT3 mutationsQ40099203
Potentiation of antileukemic therapies by Smac mimetic, LBW242: effects on mutant FLT3-expressing cellsQ40109450
4-Amino-6-piperazin-1-yl-pyrimidine-5-carbaldehyde oximes as potent FLT-3 inhibitorsQ40111543
BH3 mimetic ABT-737 neutralizes resistance to FLT3 inhibitor treatment mediated by FLT3-independent expression of BCL2 in primary AML blasts.Q40122807
The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitorsQ40182316
DNA repair contributes to the drug-resistant phenotype of primary acute myeloid leukaemia cells with FLT3 internal tandem duplications and is reversed by the FLT3 inhibitor PKC412.Q40215417
Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathwaysQ40218888
The antitumor effects of sunitinib (formerly SU11248) against a variety of human hematologic malignancies: enhancement of growth inhibition via inhibition of mammalian target of rapamycin signalingQ40220256
Constitutively activated FLT3 phosphorylates BAD partially through pim-1.Q40251345
Splenic endothelial cell lines support development of dendritic cells from bone marrow.Q40268728
Antineoplastic effect of a single oral dose of the novel Flt3 inhibitor KRN383 on xenografted human leukemic cells harboring Flt3-activating mutationsQ40294499
Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemiaQ40296363
Point mutations in the juxtamembrane domain of FLT3 define a new class of activating mutations in AML.Q40330454
Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domainQ40390558
CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma.Q40480723
RNAi-induced down-regulation of FLT3 expression in AML cell lines increases sensitivity to MLN518.Q40483270
Pim-1 is up-regulated by constitutively activated FLT3 and plays a role in FLT3-mediated cell survivalQ40501190
Identification of a novel activating mutation (Y842C) within the activation loop of FLT3 in patients with acute myeloid leukemia (AML).Q40519489
Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518.Q40534979
Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD–transformed hematopoietic cellsQ40618806
Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit.Q40659303
P433issue37
P407language of work or nameEnglishQ1860
P304page(s)5120-5134
P577publication date2010-07-12
P1433published inOncogeneQ1568657
P1476titleDrug resistance in mutant FLT3-positive AML.
P478volume29

Reverse relations

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