Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy

Emerging alternatives to tyrosine kinase inhibitors for treating chronic myeloid leukemia

(2018) Simon Kavanagh et al.   EXPERT OPINION ON EMERGING DRUGS

Bosutinib Versus Imatinib for Newly Diagnosed Chronic Myeloid Leukemia: Results From the Randomized BFORE Trial

(2018) Jorge E. Cortes et al.   JOURNAL OF CLINICAL ONCOLOGY

EzMol: A Web Server Wizard for the Rapid Visualization and Image Production of Protein and Nucleic Acid Structures

(2018) Christopher R. Reynolds et al.   JOURNAL OF MOLECULAR BIOLOGY

A new monoclonal antibody detects downregulation of protein tyrosine phosphatase receptor type γ in chronic myeloid leukemia patients

(2017) Marzia Vezzalini et al.   Journal of Hematology & Oncology

Differential signaling networks of Bcr–Abl p210 and p190 kinases in leukemia cells defined by functional proteomics

(2017) S Reckel et al.   LEUKEMIA

Design, Synthesis, and Biological Evaluation of Novel 1,3,4-Thiadiazole Derivatives as Potential Antitumor Agents against Chronic Myelogenous Leukemia: Striking Effect of Nitrothiazole Moiety

(2017) Mehlika Altıntop et al.   MOLECULES

Risk stratification of chromosomal abnormalities in chronic myelogenous leukemia in the era of tyrosine kinase inhibitor therapy

(2016) W. Wang et al.   BLOOD

Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia

(2016) Jorge Cortes et al.   HAEMATOLOGICA

European LeukemiaNet recommendations for the management and avoidance of adverse events of treatment in chronic myeloid leukaemia

(2016) J L Steegmann et al.   LEUKEMIA

Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia

(2016) Jorge Cortes et al.   HAEMATOLOGICA

Compound mutations in BCR-ABL1 are not major drivers of primary or secondary resistance to ponatinib in CP-CML patients

(2015) M. W. Deininger et al.   BLOOD

A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy

(2015) G. Borthakur et al.   HAEMATOLOGICA

Safety and efficacy of imatinib in CML over a period of 10 years: data from the randomized CML-study IV

(2015) L Kalmanti et al.   LEUKEMIA

A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy

(2015) G. Borthakur et al.   HAEMATOLOGICA

Poor response to erlotinib in patients with tumors containing baseline EGFR T790M mutations found by routine clinical molecular testing

(2014) H. A. Yu et al.   ANNALS OF ONCOLOGY

BCR-ABL1 Compound Mutations Combining Key Kinase Domain Positions Confer Clinical Resistance to Ponatinib in Ph Chromosome-Positive Leukemia

(2014) Matthew S. Zabriskie et al.   CANCER CELL

SECOND-GENERATION TYROSINE KINASE INHIBITORS (TKI) AS SALVAGE THERAPY FOR RESISTANT OR INTOLERANT PATIENTS TO PRIOR TKIs

(2014) Massimo Breccia et al.   Mediterranean Journal of Hematology and Infectious Diseases

1,3,4-Thiadiazole and its Derivatives: A Review on Recent Progress in Biological Activities

(2013) Abhishek Kumar Jain et al.   Chemical Biology & Drug Design

The background, discovery and clinical development of BCR-ABL inhibitors

(2013) Gemma K. Lambert et al.   DRUG DISCOVERY TODAY

Heterogeneity of Genetic Changes Associated with Acquired Crizotinib Resistance in ALK-Rearranged Lung Cancer

(2013) Soyeon Kim et al.   Journal of Thoracic Oncology

NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors

(2013) L. Skora et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

NI-1: a novel canine mastocytoma model for studying drug resistance and IgER-dependent mast cell activation

(2012) E. Hadzijusufovic et al.   ALLERGY

Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors

(2012) Damien Y. Duveau et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism

(2012) Mamduh Khateb et al.   BMC CANCER

BCR/ABL1 Fusion Transcripts Generated from Alternative Splicing: Implications for Future Targeted Therapies in Ph+ Leukaemias

(2012) P. Chiarella et al.   CURRENT MOLECULAR MEDICINE

Danusertib, an aurora kinase inhibitor

(2012) Hielke J Meulenbeld et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Ponatinib is active against imatinib-resistant mutants of FIP1L1-PDGFRA and KIT and against FGFR1-derived fusion kinases

(2012) E Lierman et al.   LEUKEMIA

MK-0457, an Aurora kinase and BCR–ABL inhibitor, is active in patients with BCR–ABL T315I leukemia

(2012) F J Giles et al.   LEUKEMIA

Ponatinib in Refractory Philadelphia Chromosome–Positive Leukemias

(2012) Jorge E. Cortes et al.   NEW ENGLAND JOURNAL OF MEDICINE

Predicting complete cytogenetic response and subsequent progression-free survival in 2060 patients with CML on imatinib treatment: the EUTOS score

(2011) J. Hasford et al.   BLOOD

Dasatinib or imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: 2-year follow-up from a randomized phase 3 trial (DASISION)

(2011) H. M. Kantarjian et al.   BLOOD

Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036

(2011) Wayne W. Chan et al.   CANCER CELL

The ABL Switch Control Inhibitor DCC-2036 Is Active against the Chronic Myeloid Leukemia Mutant BCR-ABLT315I and Exhibits a Narrow Resistance Profile

(2011) C. A. Eide et al.   CANCER RESEARCH

Nilotinib versus imatinib for the treatment of patients with newly diagnosed chronic phase, Philadelphia chromosome-positive, chronic myeloid leukaemia: 24-month minimum follow-up of the phase 3 randomised ENESTnd trial

(2011) Hagop M Kantarjian et al.   LANCET ONCOLOGY

Potent Activity of Ponatinib (AP24534) in Models of FLT3-Driven Acute Myeloid Leukemia and Other Hematologic Malignancies

(2011) J. M. Gozgit et al.   MOLECULAR CANCER THERAPEUTICS

An Integrated Chemical Biology Approach Identifies Specific Vulnerability of Ewing's Sarcoma to Combined Inhibition of Aurora Kinases A and B

(2011) G. E. Winter et al.   MOLECULAR CANCER THERAPEUTICS

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

(2010) E. Weisberg et al.   BLOOD

Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance

(2010) Tianjun Zhou et al.   Chemical Biology & Drug Design

Bosutinib: A review of preclinical studies in chronic myelogenous leukaemia

(2010) Frank Boschelli et al.   EUROPEAN JOURNAL OF CANCER

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

(2010) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

(2010) Jianming Zhang et al.   NATURE

The discovery of the potent aurora inhibitor MK-0457 (VX-680)

(2009) David Bebbington et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Epidemiologic study on survival of chronic myeloid leukemia and Ph+ acute lymphoblastic leukemia patients with BCR-ABL T315I mutation

(2009) F. E. Nicolini et al.   BLOOD

Mechanisms of Sunitinib Resistance in Gastrointestinal Stromal Tumors Harboring KITAY502-3ins Mutation: An In vitro Mutagenesis Screen for Drug Resistance

(2009) T. Guo et al.   CLINICAL CANCER RESEARCH

Hypereosinophilic syndrome: A multicenter, retrospective analysis of clinical characteristics and response to therapy

(2009) Princess U. Ogbogu et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Nilotinib concentration in cell lines and primary CD34+ chronic myeloid leukemia cells is not mediated by active uptake or efflux by major drug transporters

(2009) A Davies et al.   LEUKEMIA

A comprehensive target selectivity survey of the BCR-ABL kinase inhibitor INNO-406 by kinase profiling and chemical proteomics in chronic myeloid leukemia cells

(2009) U Rix et al.   LEUKEMIA

Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I

(2008) A. Gontarewicz et al.   BLOOD

Characteristics and outcomes of patients with chronic myeloid leukemia and T315I mutation following failure of imatinib mesylate therapy

(2008) E. Jabbour et al.   BLOOD

Patients' age and BCR-ABL frequency in adult B-precursor ALL: a retrospective analysis from the GMALL study group

(2008) T. Burmeister et al.   BLOOD

Activity of Dasatinib, a Dual SRC/ABL Kinase Inhibitor, and IPI-504, a Heat Shock Protein 90 Inhibitor, against Gastrointestinal Stromal Tumor-Associated PDGFRAD842V Mutation

(2008) B. Dewaele et al.   CLINICAL CANCER RESEARCH

Activity of Bosutinib, Dasatinib, and Nilotinib Against 18 Imatinib-Resistant BCR/ABL Mutants

(2008) Sara Redaelli et al.   JOURNAL OF CLINICAL ONCOLOGY

Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells

(2008) L L Remsing Rix et al.   LEUKEMIA

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY

Activation of tyrosine kinases by mutation of the gatekeeper threonine

(2008) Mohammad Azam et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Concomitant translocation t(14;22)(q32;q11) in a case of chronic myeloid leukemia

(2007) Enrico Orciuolo et al.   LEUKEMIA RESEARCH

Complex translocation t(6;9;22)(p21.1;q34;q11) at diagnosis is a therapy resistance index in chronic myeloid leukaemia

(2007) Enrico Orciuolo et al.   LEUKEMIA RESEARCH