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Chemical Biology & Drug Design, ISSN 1747-0277, 01/2011, Volume 77, Issue 1, pp. 1 - 11
The BCR‐ABL inhibitor imatinib has revolutionized the treatment of chronic myeloid leukemia. However, drug resistance caused by kinase domain mutations has... 
kinase | ponatinib | AP24534 | drug discovery | X‐ray crystallography | structure‐based drug design | X-ray crystallography | Structure-based drug design | Drug discovery | Ponatinib | Kinase | structure-based drug design | C-ABL | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | BMS-354825 | DOMAIN MUTATIONS | CANCER | CHRONIC MYELOID-LEUKEMIA | STRATEGIES | THERAPY | IMATINIB | T315I MUTANT | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - genetics | Crystallography, X-Ray | Piperazines - chemistry | Structure-Activity Relationship | Pyridazines - pharmacology | Pyridazines - chemical synthesis | Pyrimidines - chemistry | Protein Kinase Inhibitors - chemistry | Protein Binding - drug effects | Imidazoles - chemical synthesis | Imidazoles - therapeutic use | Pyridazines - therapeutic use | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology | Imidazoles - pharmacology | Piperazines - therapeutic use | Pyrimidines - pharmacology | Imatinib Mesylate | Piperazines - pharmacology | Drug Resistance, Neoplasm - genetics | Fusion Proteins, bcr-abl - genetics | Animals | Mutation - drug effects | Protein Kinase Inhibitors - therapeutic use | Pyrimidines - therapeutic use | Fusion Proteins, bcr-abl - antagonists & inhibitors | Cell Line, Tumor | Mice | Protein Kinase Inhibitors - pharmacology | Benzamides | Fluoroimmunoassay | Fusion Proteins, bcr-abl - metabolism | Drug Resistance, Neoplasm - drug effects | Drug resistance | Analysis | Leukemia | STRUCTURE-ACTIVITY RELATIONSHIPS | MUTANTS | BASIC BIOLOGICAL SCIENCES | ENZYME INHIBITORS | TYROSINE | GENE MUTATIONS | PHOSPHOTRANSFERASES | MYELOID LEUKEMIA | MUTATIONS | ANTINEOPLASTIC DRUGS | 60 APPLIED LIFE SCIENCES | RESIDUES
Journal Article
Journal of the National Cancer Institute, ISSN 0027-8874, 2018, Volume 110, Issue 5, pp. 467 - 478
Background: Imatinib and second-generation tyrosine kinase inhibitors (TKIs) nilotinib and dasatinib have statistically significantly improved the life... 
CHRONIC MYELOGENOUS LEUKEMIA | MAMMALIAN TARGET | STEM-CELLS | POTENT | PONATINIB | PROTEIN | PI3K/MTOR KINASE INHIBITOR | ONCOLOGY | IMATINIB | (PI3K)/MAMMALIAN TARGET | DISCOVERY | Life Sciences | Human health and pathology | Hematology | Cancer
Journal Article
Oncotarget, ISSN 1949-2553, 10/2018, Volume 9, Issue 78, pp. 34735 - 34747
TKI resistance remains a major impediment to successful treatment of CML. In this study, we investigated the emerging modes of ponatinib resistance in... 
Chronic myeloid leukaemia | Ponatinib resistance | Compound mutation | Bcr-Abl+ cell lines | Axl
Journal Article
Cancer Cell, ISSN 1535-6108, 09/2014, Volume 26, Issue 3, pp. 305 - 306
Journal Article
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 3/2014, Volume 111, Issue 9, pp. 3550 - 3555
The acquisition of mutations within the BCR-ABL1 kinase domain is frequently associated with tyrosine kinase inhibitor (TKI) failure in chronic myeloid... 
Leukemia | Alleles | Cytogenetics | Molecular dynamics | Chronic myeloid leukemia | Inhibitory concentration 50 | Genetic mutation | Blood | Free energy | Resistance mechanisms | Ponatinib resistance | Compound mutation | CHRONIC MYELOGENOUS LEUKEMIA | CHRONIC PHASE | TYROSINE KINASE | MULTIDISCIPLINARY SCIENCES | BCR-ABL INDEPENDENCE | DOMAIN MUTATIONS | CHRONIC MYELOID-LEUKEMIA | MESYLATE RESISTANCE | SELECTIVE INHIBITOR | ponatinib resistance | IMATINIB | CYTOGENETIC RESPONSE | compound mutation | Fusion Proteins, bcr-abl - chemistry | Piperazines | Humans | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Models, Molecular | DNA Primers - genetics | Imidazoles - pharmacology | Pyridazines - pharmacology | Mutation - genetics | Imatinib Mesylate | Molecular Dynamics Simulation | Drug Resistance, Neoplasm - genetics | Fusion Proteins, bcr-abl - genetics | Pyrimidines | Analysis of Variance | Cloning, Molecular | Polymerase Chain Reaction | Benzamides | Imidazoles - therapeutic use | Pyridazines - therapeutic use | Protein-Tyrosine Kinases - antagonists & inhibitors | Care and treatment | Molecular genetics | Gene mutations | Myelocytic leukemia | Physiological aspects | Genetic research | Genetic aspects | Nonlymphoid leukemia | Research | Phosphotransferases | Health aspects | Cancer | Biological Sciences
Journal Article
ACS CHEMICAL BIOLOGY, ISSN 1554-8929, 09/2019, Volume 14, Issue 9, pp. 1888 - 1895
We present a rapid and high-throughput yeast and flow cytometry based method for predicting kinase inhibitor resistance mutations and determining kinase... 
BCR-ABL1 COMPOUND MUTATIONS | MUTAGENESIS | PONATINIB | BIOCHEMISTRY & MOLECULAR BIOLOGY | IMATINIB | COMPLEXITY | BMS-354825 | AMN107 | ABL | NILOTINIB | CHRONIC MYELOID-LEUKEMIA
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 11/2018, Volume 24, Issue 21, pp. 5321 - 5334
Purpose: Sequential treatment with targeted therapies can result in complex combinations of resistance mutations in drug targets. This mutational complexity... 
CHRONIC MYELOGENOUS LEUKEMIA | HYPER-CVAD | PONATINIB | ONCOLOGY | KINASE DOMAIN MUTATIONS | TYROSINE KINASE | ACUTE LYMPHOBLASTIC-LEUKEMIA | COMPOUND MUTATIONS | INHIBITOR | IMATINIB MESYLATE | CHRONIC MYELOID-LEUKEMIA
Journal Article
Molecular Pharmaceutics, ISSN 1543-8384, 10/2017, Volume 14, Issue 10, pp. 3258 - 3268
Journal Article
International Journal of Biological Macromolecules, ISSN 0141-8130, 08/2019, Volume 135, pp. 294 - 302
Novel efficacious treatment of Rhabdomyosarcoma (RMS) with less toxicity has yet to emerge. Genomic analysis of RMS has reported that the receptor tyrosine... 
MD simulations | Ponatinib | Drug resistance | Umbrella sampling | MM-GBSA | Rhabdomyosarcoma | SURVIVAL | POLYMER SCIENCE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CLASSIFICATION | PARAMETERS | TUMORS | HISTOGRAM ANALYSIS METHOD | PREDICTION | DYNAMICS SIMULATIONS | CHAIN | AMBER | GENES | CHEMISTRY, APPLIED | Tyrosine | Phenols | Genetic aspects | Models | Analysis
Journal Article
Journal of Biomolecular Structure and Dynamics, ISSN 0739-1102, 2019, pp. 1 - 12
Acute lymphocytic leukemia (ALL) is one of the most dangerous types of leukemia, and about 40% of them is Philadelphia chromosome-positive acute lymphocytic... 
tyrosine kinase inhibitors | ponatinib | Acute lymphocytic leukemia | drug resistance | BCR-ABL | molecular dynamics simulation
Journal Article
HEMATOLOGICAL ONCOLOGY, ISSN 0278-0232, 12/2017, Volume 35, Issue 4, pp. 420 - 423
In the past decade, the treatment of chronic myeloid leukemia (CML) has undergone a drastic evolution. The discovery and success of imatinib and... 
STEM-CELLS | CML | leukemic stem cells | HUMAN-CELLS | DASATINIB | DISCONTINUATION | tyrosine kinase inhibitors | resistance to treatment | PONATINIB | THERAPY | ONCOLOGY | ACUTE LYMPHOBLASTIC-LEUKEMIA | IMATINIB | chronic myeloid leukemia | MUTATIONS | HEMATOLOGY
Journal Article