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Mechanisms of resistance to FLT3 inhibitors.
scientific article published on 21 January 2009
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Europe PubMed Central
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4891941
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20 January 2020
review article
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Europe PubMed Central
title
Mechanisms of resistance to FLT3 inhibitors
(English)
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Europe PubMed Central
PMCID
4891941
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:19162530%20AND%20SRC:MED&resulttype=core&format=json
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20 January 2020
author
S Haihua Chu
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1
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Europe PubMed Central
PMCID
4891941
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:19162530%20AND%20SRC:MED&resulttype=core&format=json
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20 January 2020
author name string
Donald Small
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2
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Europe PubMed Central
PMCID
4891941
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20 January 2020
publication date
21 January 2009
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Europe PubMed Central
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4891941
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20 January 2020
published in
Drug Resistance Updates
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4891941
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20 January 2020
volume
12
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PMCID
4891941
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20 January 2020
issue
1-2
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stated in
Europe PubMed Central
PMCID
4891941
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:19162530%20AND%20SRC:MED&resulttype=core&format=json
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20 January 2020
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8-16
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Europe PubMed Central
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4891941
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20 January 2020
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PML/RARalpha and FLT3-ITD induce an APL-like disease in a mouse model
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FLT3 regulates beta-catenin tyrosine phosphorylation, nuclear localization, and transcriptional activity in acute myeloid leukemia cells
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BH3 mimetic ABT-737 neutralizes resistance to FLT3 inhibitor treatment mediated by FLT3-independent expression of BCL2 in primary AML blasts.
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Over-expression of Flt3 induces NF-kappaB pathway and increases the expression of IL-6.
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MDR1 and MRP1 gene expression are independent predictors for treatment outcome in adult acute myeloid leukaemia.
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Flt3 tandem duplication mutations cooperate with Wnt signaling in leukemic signal transduction.
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In vitro studies of a FLT3 inhibitor combined with chemotherapy: sequence of administration is important to achieve synergistic cytotoxic effects
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Internal tandem duplication mutation of FLT3 blocks myeloid differentiation through suppression of C/EBPα expression
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FLT3 ligand causes autocrine signaling in acute myeloid leukemia cells
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Sensitivity toward tyrosine kinase inhibitors varies between different activating mutations of the FLT3 receptor.
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PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
14 September 2017
Several Bcr-Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
14 September 2017
FLT3 internal tandem duplication mutations associated with human acute myeloid leukemias induce myeloproliferative disease in a murine bone marrow transplant model
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
28 September 2017
In vivo treatment of mutant FLT3-transformed murine leukemia with a tyrosine kinase inhibitor
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
28 September 2017
A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
26 June 2018
Several types of mutations of the Abl gene can be found in chronic myeloid leukemia patients resistant to STI571, and they can pre-exist to the onset of treatment.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
26 June 2018
beta-Catenin is essential for survival of leukemic stem cells insensitive to kinase inhibition in mice with BCR-ABL-induced chronic myeloid leukemia
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Expansion of Bcr-Abl-positive leukemic stem cells is dependent on Hedgehog pathway activation
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
An activating KRAS mutation in imatinib-resistant chronic myeloid leukemia
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptor
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Blockade of MEK/ERK signaling enhances sunitinib-induced growth inhibition and apoptosis of leukemia cells possessing activating mutations of the FLT3 gene
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Synergistic antileukemic effects between ABT-869 and chemotherapy involve downregulation of cell cycle-regulated genes and c-Mos-mediated MAPK pathway
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Pharmacologic inhibition of CDK4/6: mechanistic evidence for selective activity or acquired resistance in acute myeloid leukemia.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Mutations of the BCR-ABL-kinase domain occur in a minority of patients with stable complete cytogenetic response to imatinib.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Not all imatinib resistance in CML are BCR-ABL kinase domain mutations.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Anticancer therapeutics: "Addictive" targets, multi-targeted drugs, new drug combinations
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Targeting NF-kappaB activation via pharmacologic inhibition of IKK2-induced apoptosis of human acute myeloid leukemia cells.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Acquisition of FLT3 or N-ras mutations is frequently associated with progression of myelodysplastic syndrome to acute myeloid leukemia
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Constitutive NF-κB DNA-binding activity in AML is frequently mediated by a Ras/PI3-K/PKB-dependent pathway
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
FLT3 mutations do not influence MDR-1 gene expression in acute myeloid leukemia.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
SU5416, a small molecule tyrosine kinase receptor inhibitor, has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
A model of APL with FLT3 mutation is responsive to retinoic acid and a receptor tyrosine kinase inhibitor, SU11657.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
BCR-ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
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.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Identification of novel FLT-3 Asp835 mutations in adult acute myeloid leukaemia
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
2 September 2018
Adaptive secretion of granulocyte-macrophage colony-stimulating factor (GM-CSF) mediates imatinib and nilotinib resistance in BCR/ABL+ progenitors via JAK-2/STAT-5 pathway activation
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
3 December 2018
A phase 2 clinical study of SU5416 in patients with refractory acute myeloid leukemia
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
3 December 2018
Expression of the hematopoietic growth factor receptor FLT3 (STK-1/Flk2) in human leukemias
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4891941
retrieved
3 December 2018
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
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/19162530
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Stability and prognostic influence of FLT3 mutations in paired initial and relapsed AML samples
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/19162530
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Internal tandem duplication of the flt3 gene found in acute myeloid leukemia
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/19162530
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
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 inhibitors
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/19162530
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Flt3high and Flt3low CD34+ progenitor cells isolated from human bone marrow are functionally distinct
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/19162530
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Preclinical targeting of NF-kappaB and FLT3 pathways in AML cells
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/19162530
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Deregulation and cross talk among Sonic hedgehog, Wnt, Hox and Notch signaling in chronic myeloid leukemia progression
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/19162530
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Identifiers
DOI
10.1016/J.DRUP.2008.12.001
1 reference
stated in
Europe PubMed Central
PMCID
4891941
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:19162530%20AND%20SRC:MED&resulttype=core&format=json
retrieved
20 January 2020
PMCID
4891941
1 reference
stated in
Europe PubMed Central
PMCID
4891941
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:19162530%20AND%20SRC:MED&resulttype=core&format=json
retrieved
20 January 2020
PubMed ID
19162530
1 reference
stated in
Europe PubMed Central
PMCID
4891941
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:19162530%20AND%20SRC:MED&resulttype=core&format=json
retrieved
20 January 2020
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