FLT3 inhibition: a moving and evolving target in acute myeloid leukaemia (Q38026453)

27 August 2017

FLT3 inhibition: a moving and evolving target in acute myeloid leukaemia (English)

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27 August 2017

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A Y H Leung

1

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27 August 2017

C-H Man

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2

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27 August 2017

Y-L Kwong

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3

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27 August 2017

16 July 2012

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27 August 2017

9

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inferred from page(s)

published in

Leukemia

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27 August 2017

27

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27 August 2017

2

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27 August 2017

260-268

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https://scigraph.springernature.com/pub.10.1038/leu.2012.195

27 August 2017

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Analysis of FLT3 length mutations in 1003 patients with acute myeloid leukemia: correlation to cytogenetics, FAB subtype, and prognosis in the AMLCG study and usefulness as a marker for the detection of minimal residual disease

21 January 2018

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Structural and functional alterations of FLT3 in acute myeloid leukemia

21 January 2018

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A receptor tyrosine kinase specific to hematopoietic stem and progenitor cell-enriched populations

21 January 2018

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AML-associated Flt3 kinase domain mutations show signal transduction differences compared with Flt3 ITD mutations.

21 January 2018

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Roles of tyrosine 589 and 591 in STAT5 activation and transformation mediated by FLT3-ITD.

21 January 2018

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SRC is a signaling mediator in FLT3-ITD- but not in FLT3-TKD-positive AML.

21 January 2018

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Constitutive activation of Akt by Flt3 internal tandem duplications is necessary for increased survival, proliferation, and myeloid transformation.

21 January 2018

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FLT3-ITD induces ara-C resistance in myeloid leukemic cells through the repression of the ENT1 expression

21 January 2018

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Internal tandem duplication of FLT3 (FLT3/ITD) induces increased ROS production, DNA damage, and misrepair: implications for poor prognosis in AML.

21 January 2018

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Cell cycle regulation by oncogenic tyrosine kinases in myeloid neoplasias: from molecular redox mechanisms to health implications

21 January 2018

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Signal transduction of oncogenic Flt3.

21 January 2018

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Targeting FLT3 for the treatment of leukemia

21 January 2018

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The role of FLT3 in haematopoietic malignancies

21 January 2018

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Clinical significance of FLT3 in leukemia

21 January 2018

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Structural and numerical variation of FLT3/ITD in pediatric AML.

21 January 2018

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Prognostic value of FLT3 mutations among different cytogenetic subgroups in acute myeloid leukemia

21 January 2018

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The impact of FLT3 internal tandem duplication mutant level, number, size, and interaction with NPM1 mutations in a large cohort of young adult patients with acute myeloid leukemia

21 January 2018

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FLT3 inhibitors in the treatment of acute myeloid leukemia: the start of an era?

21 January 2018

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FLT3 as a therapeutic target in AML: still challenging after all these years

21 January 2018

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FLT3 inhibition in acute myeloid leukaemia

21 January 2018

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The clinical development of FLT3 inhibitors in acute myeloid leukemia

21 January 2018

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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.

21 January 2018

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Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

p53 activation of mesenchymal stromal cells partially abrogates microenvironment-mediated resistance to FLT3 inhibition in AML through HIF-1α-mediated down-regulation of CXCL12.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Stromal niche cells protect early leukemic FLT3-ITD+ progenitor cells against first-generation FLT3 tyrosine kinase inhibitors.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Mechanisms of resistance against PKC412 in resistant FLT3-ITD positive human acute myeloid leukemia cells

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Drug resistance in mutant FLT3-positive AML.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

A novel molecular mechanism of primary resistance to FLT3-kinase inhibitors in AML.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Clonal evolution in cancer

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Part I: mechanisms of resistance to imatinib in chronic myeloid leukaemia

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Cancer stem cells in solid tumours: accumulating evidence and unresolved questions

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

The presence of a FLT3 internal tandem duplication in patients with acute myeloid leukemia (AML) adds important prognostic information to cytogenetic risk group and response to the first cycle of chemotherapy: analysis of 854 patients from the Unite

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Internal tandem duplications of the FLT3 gene are present in leukemia stem cells

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Knock-in of a FLT3/ITD mutation cooperates with a NUP98-HOXD13 fusion to generate acute myeloid leukemia in a mouse model

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Can FLT3 inhibitors overcome resistance in AML?

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Results from a randomized trial of salvage chemotherapy followed by lestaurtinib for patients with FLT3 mutant AML in first relapse

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Phase 1 clinical results with tandutinib (MLN518), a novel FLT3 antagonist, in patients with acute myelogenous leukemia or high-risk myelodysplastic syndrome: safety, pharmacokinetics, and pharmacodynamics

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

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 disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Mutant FLT3: a direct target of sorafenib in acute myelogenous leukemia

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Phase I/II study of combination therapy with sorafenib, idarubicin, and cytarabine in younger patients with acute myeloid leukemia

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

FLT3-ITD and tyrosine kinase domain mutants induce 2 distinct phenotypes in a murine bone marrow transplantation model

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Molecular mechanisms of resistance to imatinib in Philadelphia-chromosome-positive leukaemias.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Identification of a secondary FLT3/A848P mutation in a patient with FLT3-ITD-positive blast phase CMML and response to sunitinib and sorafenib

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Clonal evolution in relapsed acute myeloid leukaemia revealed by whole-genome sequencing

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Selective FLT3 inhibitor FI-700 neutralizes Mcl-1 and enhances p53-mediated apoptosis in AML cells with activating mutations of FLT3 through Mcl-1/Noxa axis

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Tyrosine kinase inhibitors for the treatment of acute myeloid leukemia: delineation of anti-leukemic mechanisms of action

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Sensitivity toward tyrosine kinase inhibitors varies between different activating mutations of the FLT3 receptor.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

FLT3-ITD-TKD dual mutants associated with AML confer resistance to FLT3 PTK inhibitors and cytotoxic agents by overexpression of Bcl-x(L).

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Ponatinib may overcome resistance of FLT3-ITD harbouring additional point mutations, notably the previously refractory F691I mutation

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

Nuclear factor-kappaB is constitutively activated in primitive human acute myelogenous leukemia cells

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

The sesquiterpene lactone parthenolide induces apoptosis of human acute myelogenous leukemia stem and progenitor cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Targeting NF-kappaB activation via pharmacologic inhibition of IKK2-induced apoptosis of human acute myeloid leukemia cells.

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

A potential therapeutic target for FLT3-ITD AML: PIM1 kinase

21 January 2018

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https://api.crossref.org/works/10.1038%2FLEU.2012.195

MS-275, a novel histone deacetylase inhibitor with selectivity against HDAC1, induces degradation of FLT3 via inhibition of chaperone function of heat shock protein 90 in AML cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Heat shock protein 90 inhibition is cytotoxic to primary AML cells expressing mutant FLT3 and results in altered downstream signalling.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Compassionate use of sorafenib in FLT3-ITD-positive acute myeloid leukemia: sustained regression before and after allogeneic stem cell transplantation

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

A pharmacodynamic study of sorafenib in patients with relapsed and refractory acute leukemias

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

SU5416, a small molecule tyrosine kinase receptor inhibitor, has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Identification of novel FLT-3 Asp835 mutations in adult acute myeloid leukaemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Analysis of FLT3-activating mutations in 979 patients with acute myelogenous leukemia: association with FAB subtypes and identification of subgroups with poor prognosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Clinical impact of internal tandem duplications and activating point mutations in FLT3 in acute myeloid leukemia in elderly patients.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Mutations of the FLT3 gene in adult acute myeloid leukemia: determination of incidence and identification of a novel mutation in a Thai population

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Prognostic relevance of FLT3-TKD mutations in AML: the combination matters--an analysis of 3082 patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

FLT3 D835/I836 mutations are associated with poor disease-free survival and a distinct gene-expression signature among younger adults with de novo cytogenetically normal acute myeloid leukemia lacking FLT3 internal tandem duplications

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

The multitargeted receptor tyrosine kinase inhibitor linifanib (ABT-869) induces apoptosis through an Akt and glycogen synthase kinase 3β-dependent pathway.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Discovery of LY2457546: a multi-targeted anti-angiogenic kinase inhibitor with a novel spectrum of activity and exquisite potency in the acute myelogenous leukemia-Flt-3-internal tandem duplication mutant human tumor xenograft model.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Combination of rapamycin and protein tyrosine kinase (PTK) inhibitors for the treatment of leukemias caused by oncogenic PTKs

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

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 signaling

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Blockade of MEK/ERK signaling enhances sunitinib-induced growth inhibition and apoptosis of leukemia cells possessing activating mutations of the FLT3 gene

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Combining the FLT3 inhibitor PKC412 and the triterpenoid CDDO-Me synergistically induces apoptosis in acute myeloid leukemia with the internal tandem duplication mutation

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

PRL-3, a metastasis associated tyrosine phosphatase, is involved in FLT3-ITD signaling and implicated in anti-AML therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Novel targeted therapy for acute myeloid leukemia with a dual FLT3 and JAK2 inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

A phase 2 clinical study of SU5416 in patients with refractory acute myeloid leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

Internal tandem duplication of the FLT3 gene is a novel modality of elongation mutation which causes constitutive activation of the product

21 January 2018

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Internal tandem duplication of FLT3 associated with leukocytosis in acute promyelocytic leukemia. Leukemia Study Group of the Ministry of Health and Welfare (Kohseisho)

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Prognostic significance of FLT3 ITD and D835 mutations in AML patients

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Internal tandem duplication of FLT3 in relapsed acute myeloid leukemia: a comparative analysis of bone marrow samples from 108 adult patients at diagnosis and relapse

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

FLT3/internal tandem duplication subclones in acute myeloid leukemia differ in their engraftment potential in NOD/SCID mice

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Phase IB study of the FLT3 kinase inhibitor midostaurin with chemotherapy in younger newly diagnosed adult patients with acute myeloid leukemia

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

AS602868, a dual inhibitor of IKK2 and FLT3 to target AML cells

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Synergistic effect of arsenic trioxide and flt3 inhibition on cells with flt3 internal tandem duplication

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors.

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

High activity of sorafenib in FLT3-ITD-positive acute myeloid leukemia synergizes with allo-immune effects to induce sustained responses.

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Analysis of FLT3 internal tandem duplication and D835 mutations in Chinese acute leukemia patients

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

FLT3 tyrosine kinase domain mutations are biologically distinct from and have a significantly more favorable prognosis than FLT3 internal tandem duplications in patients with acute myeloid leukemia

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

SKLB1028, a novel oral multikinase inhibitor of EGFR, FLT3 and Abl, displays exceptional activity in models of FLT3-driven AML and considerable potency in models of CML harboring Abl mutants.

1 reference

https://api.crossref.org/works/10.1038%2FLEU.2012.195

7 January 2021

Identifiers

DOI

10.1038/LEU.2012.195

1 reference

Dimensions Publication ID

27 August 2017

0 references

1 reference