Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy
Published 2018 View Full Article
- Home
- Publications
- Publication Search
- Publication Details
Title
Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy
Authors
Keywords
Bcr-Abl, Structure-activity relationship, Leukemia, Targeted therapy, Tyrosine kinase inhibitors (TKIs), Imatinib, Dasatinib, Nilotinib, Bosutinib, Ponatinib
Journal
Journal of Hematology & Oncology
Volume 11, Issue 1, Pages -
Publisher
Springer Nature
Online
2018-06-20
DOI
10.1186/s13045-018-0624-2
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- 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
Add your recorded webinar
Do you already have a recorded webinar? Grow your audience and get more views by easily listing your recording on Peeref.
Upload NowBecome a Peeref-certified reviewer
The Peeref Institute provides free reviewer training that teaches the core competencies of the academic peer review process.
Get Started