1
|
Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis.
|
Cancer Cell
|
2005
|
17.41
|
2
|
A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome.
|
N Engl J Med
|
2003
|
11.17
|
3
|
Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL.
|
N Engl J Med
|
2006
|
8.26
|
4
|
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.
|
Cancer Cell
|
2005
|
7.99
|
5
|
The roles of FLT3 in hematopoiesis and leukemia.
|
Blood
|
2002
|
6.14
|
6
|
Growth suppression of pre-T acute lymphoblastic leukemia cells by inhibition of notch signaling.
|
Mol Cell Biol
|
2003
|
4.43
|
7
|
Tumor cell-specific bioluminescence platform to identify stroma-induced changes to anticancer drug activity.
|
Nat Med
|
2010
|
4.00
|
8
|
Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412.
|
Blood
|
2004
|
3.84
|
9
|
Inhibition of FLT3 in MLL. Validation of a therapeutic target identified by gene expression based classification.
|
Cancer Cell
|
2003
|
3.75
|
10
|
PDGFRs are critical for PI3K/Akt activation and negatively regulated by mTOR.
|
J Clin Invest
|
2007
|
3.54
|
11
|
The JAK2V617F activating mutation occurs in chronic myelomonocytic leukemia and acute myeloid leukemia, but not in acute lymphoblastic leukemia or chronic lymphocytic leukemia.
|
Blood
|
2005
|
3.48
|
12
|
c-MET mutational analysis in small cell lung cancer: novel juxtamembrane domain mutations regulating cytoskeletal functions.
|
Cancer Res
|
2003
|
3.39
|
13
|
Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia.
|
Nat Rev Cancer
|
2007
|
3.36
|
14
|
High-throughput sequence analysis of the tyrosine kinome in acute myeloid leukemia.
|
Blood
|
2008
|
3.30
|
15
|
Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles.
|
Cancer Cell
|
2007
|
3.23
|
16
|
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412.
|
Cancer Cell
|
2002
|
3.09
|
17
|
PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease.
|
Cancer Cell
|
2003
|
2.70
|
18
|
Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia.
|
Proc Natl Acad Sci U S A
|
2009
|
2.54
|
19
|
Epidermal growth factor-independent transformation of Ba/F3 cells with cancer-derived epidermal growth factor receptor mutants induces gefitinib-sensitive cell cycle progression.
|
Cancer Res
|
2005
|
2.49
|
20
|
Critical role for Gab2 in transformation by BCR/ABL.
|
Cancer Cell
|
2002
|
2.42
|
21
|
t(11;19)(q21;p13) translocation in mucoepidermoid carcinoma creates a novel fusion product that disrupts a Notch signaling pathway.
|
Nat Genet
|
2003
|
2.30
|
22
|
The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors.
|
Blood
|
2011
|
2.23
|
23
|
The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo.
|
Blood
|
2005
|
2.14
|
24
|
Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study.
|
Blood
|
2007
|
1.85
|
25
|
Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias.
|
Blood
|
2006
|
1.83
|
26
|
Combination of rapamycin and protein tyrosine kinase (PTK) inhibitors for the treatment of leukemias caused by oncogenic PTKs.
|
Proc Natl Acad Sci U S A
|
2004
|
1.82
|
27
|
Activation of the PI3K/mTOR pathway by BCR-ABL contributes to increased production of reactive oxygen species.
|
Blood
|
2004
|
1.81
|
28
|
Identification of a family of mastermind-like transcriptional coactivators for mammalian notch receptors.
|
Mol Cell Biol
|
2002
|
1.81
|
29
|
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder.
|
Proc Natl Acad Sci U S A
|
2004
|
1.81
|
30
|
Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia.
|
Cancer Res
|
2004
|
1.79
|
31
|
The Notch coactivator, MAML1, functions as a novel coactivator for MEF2C-mediated transcription and is required for normal myogenesis.
|
Genes Dev
|
2006
|
1.79
|
32
|
BCR/ABL induces expression of vascular endothelial growth factor and its transcriptional activator, hypoxia inducible factor-1alpha, through a pathway involving phosphoinositide 3-kinase and the mammalian target of rapamycin.
|
Blood
|
2002
|
1.62
|
33
|
AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia.
|
Clin Cancer Res
|
2005
|
1.61
|
34
|
Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412.
|
Blood
|
2005
|
1.58
|
35
|
The Jak2V617F oncogene associated with myeloproliferative diseases requires a functional FERM domain for transformation and for expression of the Myc and Pim proto-oncogenes.
|
Blood
|
2008
|
1.55
|
36
|
Role of FLT3 in leukemia.
|
Curr Opin Hematol
|
2002
|
1.52
|
37
|
Transforming activity of MECT1-MAML2 fusion oncoprotein is mediated by constitutive CREB activation.
|
EMBO J
|
2005
|
1.48
|
38
|
FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML.
|
Drug Resist Updat
|
2009
|
1.47
|
39
|
NOTCH2 and FLT3 gene mis-splicings are common events in patients with acute myeloid leukemia (AML): new potential targets in AML.
|
Blood
|
2014
|
1.44
|
40
|
Inhibition of notch signaling blocks growth of glioblastoma cell lines and tumor neurospheres.
|
Genes Cancer
|
2010
|
1.33
|
41
|
The notch regulator MAML1 interacts with p53 and functions as a coactivator.
|
J Biol Chem
|
2007
|
1.33
|
42
|
Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants.
|
Blood
|
2010
|
1.32
|
43
|
FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies.
|
Oncogene
|
2005
|
1.32
|
44
|
Activated Jak2 with the V617F point mutation promotes G1/S phase transition.
|
J Biol Chem
|
2006
|
1.31
|
45
|
Identifying and characterizing a novel activating mutation of the FLT3 tyrosine kinase in AML.
|
Blood
|
2004
|
1.27
|
46
|
Molecular mechanisms of transformation by the BCR-ABL oncogene.
|
Semin Hematol
|
2003
|
1.26
|
47
|
Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment.
|
Mini Rev Med Chem
|
2004
|
1.26
|
48
|
A robust error model for iTRAQ quantification reveals divergent signaling between oncogenic FLT3 mutants in acute myeloid leukemia.
|
Mol Cell Proteomics
|
2009
|
1.25
|
49
|
Stromal-mediated protection of tyrosine kinase inhibitor-treated BCR-ABL-expressing leukemia cells.
|
Mol Cancer Ther
|
2008
|
1.23
|
50
|
The EOL-1 cell line as an in vitro model for the study of FIP1L1-PDGFRA-positive chronic eosinophilic leukemia.
|
Blood
|
2003
|
1.22
|
51
|
NPM-ALK fusion kinase of anaplastic large-cell lymphoma regulates survival and proliferative signaling through modulation of FOXO3a.
|
Blood
|
2004
|
1.21
|
52
|
Potentiation of antileukemic therapies by Smac mimetic, LBW242: effects on mutant FLT3-expressing cells.
|
Mol Cancer Ther
|
2007
|
1.18
|
53
|
Tyrosine kinase oncogenes in normal hematopoiesis and hematological disease.
|
Oncogene
|
2002
|
1.17
|
54
|
FLT3 receptors with internal tandem duplications promote cell viability and proliferation by signaling through Foxo proteins.
|
Oncogene
|
2004
|
1.17
|
55
|
Acute myeloid leukemia and acute promyelocytic leukemia.
|
Hematology Am Soc Hematol Educ Program
|
2003
|
1.16
|
56
|
BCR-ABL promotes the frequency of mutagenic single-strand annealing DNA repair.
|
Blood
|
2009
|
1.13
|
57
|
Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity.
|
Gastroenterology
|
2006
|
1.09
|
58
|
Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells.
|
Blood
|
2008
|
1.09
|
59
|
After chronic myelogenous leukemia: tyrosine kinase inhibitors in other hematologic malignancies.
|
Blood
|
2004
|
1.09
|
60
|
Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.
|
ACS Chem Biol
|
2013
|
1.08
|
61
|
FLT3 internal tandem duplication mutations induce myeloproliferative or lymphoid disease in a transgenic mouse model.
|
Oncogene
|
2005
|
1.05
|
62
|
The STAT5 Inhibitor Pimozide Displays Efficacy in Models of Acute Myelogenous Leukemia Driven by FLT3 Mutations.
|
Genes Cancer
|
2012
|
1.05
|
63
|
The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in the bone marrow microenvironment.
|
Cancer Res
|
2002
|
1.04
|
64
|
A fragment of paxillin binds the alpha 4 integrin cytoplasmic domain (tail) and selectively inhibits alpha 4-mediated cell migration.
|
J Biol Chem
|
2002
|
1.03
|
65
|
Modulation of Notch signaling by mastermind-like (MAML) transcriptional co-activators and their involvement in tumorigenesis.
|
Semin Cancer Biol
|
2004
|
1.02
|
66
|
Structure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinases.
|
Nat Struct Mol Biol
|
2013
|
1.01
|
67
|
Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells.
|
Blood
|
2008
|
1.01
|
68
|
Retrospective real-world comparison of medical visits, costs, and adherence between nilotinib and dasatinib in chronic myeloid leukemia.
|
Curr Med Res Opin
|
2010
|
0.99
|
69
|
Effects of the Bcr/abl kinase inhibitors STI571 and adaphostin (NSC 680410) on chronic myelogenous leukemia cells in vitro.
|
Blood
|
2002
|
0.98
|
70
|
A genome-wide aberrant RNA splicing in patients with acute myeloid leukemia identifies novel potential disease markers and therapeutic targets.
|
Clin Cancer Res
|
2013
|
0.95
|
71
|
The transcriptional coactivator Maml1 is required for Notch2-mediated marginal zone B-cell development.
|
Blood
|
2007
|
0.95
|
72
|
Identification of mTOR as a novel bifunctional target in chronic myeloid leukemia: dissection of growth-inhibitory and VEGF-suppressive effects of rapamycin in leukemic cells.
|
FASEB J
|
2005
|
0.93
|
73
|
Novel oncogenic mutations of CBL in human acute myeloid leukemia that activate growth and survival pathways depend on increased metabolism.
|
J Biol Chem
|
2010
|
0.90
|
74
|
Stable expression of small interfering RNA sensitizes TEL-PDGFbetaR to inhibition with imatinib or rapamycin.
|
J Clin Invest
|
2004
|
0.90
|
75
|
The mastermind-like 1 (MAML1) co-activator regulates constitutive NF-kappaB signaling and cell survival.
|
J Biol Chem
|
2010
|
0.90
|
76
|
Discovery of a selective irreversible BMX inhibitor for prostate cancer.
|
ACS Chem Biol
|
2013
|
0.89
|
77
|
Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma.
|
ACS Chem Biol
|
2014
|
0.88
|
78
|
Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells.
|
PLoS One
|
2013
|
0.88
|
79
|
Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison.
|
Genes Cancer
|
2010
|
0.87
|
80
|
Differential expression and signaling of CBL and CBL-B in BCR/ABL transformed cells.
|
Oncogene
|
2002
|
0.87
|
81
|
The Public Repository of Xenografts Enables Discovery and Randomized Phase II-like Trials in Mice.
|
Cancer Cell
|
2016
|
0.87
|
82
|
Patupilone (epothilone B) inhibits growth and survival of multiple myeloma cells in vitro and in vivo.
|
Blood
|
2004
|
0.85
|
83
|
Following the cytokine signaling pathway to leukemogenesis: a chronology.
|
J Clin Invest
|
2008
|
0.84
|
84
|
Discovery and characterization of novel mutant FLT3 kinase inhibitors.
|
Mol Cancer Ther
|
2010
|
0.84
|
85
|
Resistance to imatinib (Glivec): update on clinical mechanisms.
|
Drug Resist Updat
|
2003
|
0.84
|
86
|
Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells.
|
PLoS One
|
2011
|
0.84
|
87
|
Cloning and functional characterization of the murine mastermind-like 1 (Maml1) gene.
|
Gene
|
2004
|
0.83
|
88
|
A retrospective analysis of therapy adherence in imatinib resistant or intolerant patients with chronic myeloid leukemia receiving nilotinib or dasatinib in a real-world setting.
|
Curr Med Res Opin
|
2012
|
0.82
|
89
|
JAK2 gets histone H3 rolling.
|
Cancer Cell
|
2009
|
0.80
|
90
|
A sensitive high-throughput method to detect activating mutations of Jak2 in peripheral-blood samples.
|
Blood
|
2006
|
0.80
|
91
|
Mutated tyrosine kinases as therapeutic targets in myeloid leukemias.
|
Adv Exp Med Biol
|
2003
|
0.79
|
92
|
Alternative splicing in chronic myeloid leukemia (CML): a novel therapeutic target?
|
Curr Cancer Drug Targets
|
2013
|
0.79
|
93
|
Wnt/β-catenin Pathway Modulates the Sensitivity of the Mutant FLT3 Receptor Kinase Inhibitors in a GSK-3β Dependent Manner.
|
Genes Cancer
|
2010
|
0.79
|
94
|
An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit.
|
Bioorg Med Chem Lett
|
2012
|
0.78
|
95
|
Aminopeptidase inhibitors inhibit proliferation and induce apoptosis of K562 and STI571-resistant K562 cell lines through the MAPK and GSK-3beta pathways.
|
Leuk Lymphoma
|
2003
|
0.78
|
96
|
Interaction maps for kinase inhibitors.
|
Nat Biotechnol
|
2005
|
0.77
|
97
|
Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.
|
Bioorg Med Chem Lett
|
2012
|
0.77
|
98
|
Combination therapy with nilotinib for drug-sensitive and drug-resistant BCR-ABL-positive leukemia and other malignancies.
|
Arch Toxicol
|
2014
|
0.76
|
99
|
The TEL/ARG leukemia oncogene promotes viability and hyperresponsiveness to hematopoietic growth factors.
|
Int J Hematol
|
2004
|
0.75
|