(Q36939898)

17 August 2017

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title

Flying under the radar: the new wave of BCR-ABL inhibitors (English)

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17 August 2017

2

Hagop Kantarjian

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17 August 2017

3

Jorge Cortes

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17 August 2017

Alfonso Quintás-Cardama

series ordinal

1

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17 August 2017

1 October 2007

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Nature Reviews Drug Discovery

17 August 2017

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17 August 2017

6

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17 August 2017

10

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17 August 2017

834-848

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https://scigraph.springernature.com/pub.10.1038/nrd2324

17 August 2017

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31 March 2020

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Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia

31 March 2020

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The conformational plasticity of protein kinases

31 March 2020

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Structural mechanism for STI-571 inhibition of abelson tyrosine kinase

31 March 2020

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Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia

31 March 2020

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Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome

31 March 2020

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Imatinib therapy in chronic myelogenous leukemia: strategies to avoid and overcome resistance

31 March 2020

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Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia

31 March 2020

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31 March 2020

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31 March 2020

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Several Bcr-Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib

31 March 2020

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

31 March 2020

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A myristoyl/phosphotyrosine switch regulates c-Abl

31 March 2020

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Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL.

31 March 2020

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Phosphorylation of the ATP-binding loop directs oncogenicity of drug-resistant BCR-ABL mutants

31 March 2020

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BCR-ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571.

31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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Dasatinib induces notable hematologic and cytogenetic responses in chronic-phase chronic myeloid leukemia after failure of imatinib therapy

31 March 2020

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Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis.

31 March 2020

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Survival benefit with imatinib mesylate versus interferon-alpha-based regimens in newly diagnosed chronic-phase chronic myelogenous leukemia

31 March 2020

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Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

31 March 2020

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Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

31 March 2020

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Overriding imatinib resistance with a novel ABL kinase inhibitor

31 March 2020

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Abl inhibitor BMS354825 binding mode in Abelson kinase revealed by molecular docking studies

31 March 2020

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The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants

31 March 2020

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Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance

31 March 2020

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31 March 2020

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In reply to 'Cardiotoxicity of the cancer therapeutic agent imatinib mesylate'

31 March 2020

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Src family tyrosine kinases and growth factor signaling

31 March 2020

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Genetic evidence for the involvement of the lck tyrosine kinase in signal transduction through the T cell antigen receptor

31 March 2020

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The interaction of the Bcr-Abl tyrosine kinase with the Src kinase Hck is mediated by multiple binding domains

31 March 2020

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Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia

31 March 2020

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The Src family kinase Hck interacts with Bcr-Abl by a kinase-independent mechanism and phosphorylates the Grb2-binding site of Bcr

31 March 2020

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The Src family kinase Hck couples BCR/ABL to STAT5 activation in myeloid leukemia cells.

31 March 2020

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Persistence of malignant hematopoietic progenitors in chronic myelogenous leukemia patients in complete cytogenetic remission following imatinib mesylate treatment

31 March 2020

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Cell cycle targets of Ras/Raf signalling

31 March 2020

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STAT5 as a molecular regulator of proliferation, differentiation and apoptosis in hematopoietic cells

31 March 2020

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A Bcr/Abl-independent, Lyn-dependent form of imatinib mesylate (STI-571) resistance is associated with altered expression of Bcl-2.

31 March 2020

1 reference

Imatinib mesylate resistance through BCR-ABL independence in chronic myelogenous leukemia

31 March 2020

1 reference

Relation between resistance of Philadelphia-chromosome-positive acute lymphoblastic leukaemia to the tyrosine kinase inhibitor STI571 and gene-expression profiles: a gene-expression study

31 March 2020

1 reference

A Src-like inactive conformation in the abl tyrosine kinase domain

31 March 2020

1 reference

Structural basis for the autoinhibition of c-Abl tyrosine kinase

31 March 2020

1 reference

In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells

31 March 2020

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Functional ABCG2 is overexpressed on primary CML CD34+ cells and is inhibited by imatinib mesylate

31 March 2020

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Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study.

31 March 2020

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NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia

31 March 2020

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In vivo antiproliferative effect of NS-187, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor, on leukemic cells harbouring Abl kinase domain mutations

31 March 2020

1 reference

INNO-406, a novel BCR-ABL/Lyn dual tyrosine kinase inhibitor, suppresses the growth of Ph+ leukemia cells in the central nervous system, and cyclosporine A augments its in vivo activity.

31 March 2020

1 reference

Low concentrations of STI571 in the cerebrospinal fluid: a case report

31 March 2020

1 reference

Imatinib mesylate has limited activity against the central nervous system involvement of Philadelphia chromosome-positive acute lymphoblastic leukaemia due to poor penetration into cerebrospinal fluid

31 March 2020

1 reference

Plasma and cerebrospinal fluid pharmacokinetics of imatinib after administration to nonhuman primates

31 March 2020

1 reference

N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor

31 March 2020

1 reference

Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds

31 March 2020

1 reference

Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases

31 March 2020

1 reference

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.

31 March 2020

1 reference

Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance

31 March 2020

1 reference

In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.

31 March 2020

1 reference

Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors

31 March 2020

1 reference

PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia

31 March 2020

1 reference

Novel compounds with antiproliferative activity against imatinib-resistant cell lines

31 March 2020

1 reference

Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation

31 March 2020

1 reference

The Src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases

31 March 2020

1 reference

Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases

31 March 2020

1 reference

Allosteric inhibitors of Bcr-abl-dependent cell proliferation

31 March 2020

1 reference

A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance

31 March 2020

1 reference

Antibody microinjection reveals an essential role for human polo-like kinase 1 (Plk1) in the functional maturation of mitotic centrosomes

31 March 2020

1 reference

ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent.

31 March 2020

1 reference

The cellular geography of aurora kinases

31 March 2020

1 reference

VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo

31 March 2020

1 reference

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

31 March 2020

1 reference

Structural basis for potent inhibition of the Aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680.

31 March 2020

1 reference

Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.

31 March 2020

1 reference

MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation

31 March 2020

1 reference

Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate

31 March 2020

1 reference

BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo.

31 March 2020

1 reference

A small molecule-kinase interaction map for clinical kinase inhibitors

31 March 2020

1 reference

BIRB-796 is not an effective ABL(T315I) inhibitor

31 March 2020

1 reference

AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes

31 March 2020

1 reference

A sequential blockade strategy for the design of combination therapies to overcome oncogene addiction in chronic myelogenous leukemia

31 March 2020

1 reference

BCR-ABL(T315I) transcript disappearance in an imatinib-resistant CML patient treated with homoharringtonine: a new therapeutic challenge?

31 March 2020

1 reference

Fusion of a kinase gene, ALK, to a nucleolar protein gene, NPM, in non-Hodgkin's lymphoma

31 March 2020

1 reference

A mutation in the RET proto-oncogene associated with multiple endocrine neoplasia type 2B and sporadic medullary thyroid carcinoma

31 March 2020

1 reference

Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors

31 March 2020

1 reference

EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy

31 March 2020

1 reference

Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib

31 March 2020

1 reference

A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient

31 March 2020

1 reference

EGFR mutation and resistance of non-small-cell lung cancer to gefitinib

31 March 2020

1 reference

A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome

31 March 2020

1 reference

The protein tyrosine kinase family of the human genome

31 March 2020

1 reference

The protein kinase complement of the human genome

31 March 2020

1 reference

Rational design of inhibitors that bind to inactive kinase conformations

31 March 2020

1 reference

Crystal structure of the tyrosine kinase domain of the human insulin receptor

31 March 2020

1 reference

Substrate competitive inhibitors of IGF-1 receptor kinase

31 March 2020

1 reference

Mitotic kinases as regulators of cell division and its checkpoints

31 March 2020

1 reference

Structure-function relationships in Src family and related protein tyrosine kinases

31 March 2020

1 reference

Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment

31 March 2020

1 reference

31 March 2020

Identifiers

DOI

10.1038/NRD2324

1 reference

PubMed ID

17853901

Dimensions Publication ID

17 August 2017

0 references

1 reference

PubMed ID

17853901