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Cancer Cell, ISSN 1535-6108, 2009, Volume 16, Issue 5, pp. 401 - 412
Inhibition of BCR-ABL by imatinib induces durable responses in many patients with chronic myeloid leukemia (CML), but resistance attributable to kinase domain... 
CHEMBIO | HUMDISEASE | CHRONIC MYELOGENOUS LEUKEMIA | DASATINIB BMS-354825 | MESYLATE | CML | ONCOLOGY | KINASE DOMAIN MUTATIONS | AMN107 | IMATINIB RESISTANCE | NILOTINIB | Proto-Oncogene Proteins c-abl - antagonists & inhibitors | Humans | Imidazoles - chemistry | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - genetics | Crystallography, X-Ray | Pyridazines - pharmacology | Protein Kinase Inhibitors - chemistry | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - pathology | Antineoplastic Agents - pharmacology | Fusion Proteins, bcr-abl - chemistry | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology | Proto-Oncogene Proteins c-abl - genetics | Cell Growth Processes - drug effects | Proto-Oncogene Proteins c-abl - chemistry | Models, Molecular | Imidazoles - pharmacology | Antineoplastic Agents - chemistry | Mice, SCID | Pyridazines - chemistry | Fusion Proteins, bcr-abl - genetics | Animals | Signal Transduction - drug effects | Fusion Proteins, bcr-abl - antagonists & inhibitors | Cell Line, Tumor | Proto-Oncogene Proteins c-abl - metabolism | Mice | Protein Kinase Inhibitors - pharmacology | Fusion Proteins, bcr-abl - metabolism | Chronic myeloid leukemia | BCR protein | Imatinib | Mutagenesis | Abl protein | Mutation | Fusion protein | Tumors | Index Medicus | imatinib resistance | dasatinib | nilotinib | compound mutation
Journal Article
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 6/2006, Volume 103, Issue 24, pp. 9244 - 9249
Mutation in the ABL kinase domain is the principal mechanism of imatinib resistance in patients with chronic myelogenous leukemia. Many mutations favor active... 
Relapse | Mutagenesis | Active sites | Mutagenicity tests | Drug regulation | Point mutation | Disease remission | Drug resistance | Preclinical drug evaluation | Cells | Chronic myelogenous leukemia | Imatinib | Kinase inhibitors | Combination chemotherapy | WILD-TYPE | C-ABL | TYROSINE KINASE | CRYSTAL-STRUCTURE | MULTIDISCIPLINARY SCIENCES | combination chemotherapy | BLAST CRISIS | imatinib | chronic myelogenous leukemia | CHRONIC MYELOID-LEUKEMIA | kinase inhibitors | STRUCTURAL BASIS | CLINICAL RESISTANCE | MUTANT BCR-ABL | Proto-Oncogene Proteins c-abl - antagonists & inhibitors | Protein-Tyrosine Kinases - metabolism | Pyridines - chemistry | Humans | Piperazines - metabolism | Piperazines - chemistry | Pyrimidines - chemistry | Pyrimidines - metabolism | Protein Kinase Inhibitors - chemistry | Protein-Tyrosine Kinases - genetics | Fusion Proteins, bcr-abl | Adenosine Triphosphate - metabolism | Drug Resistance - physiology | src-Family Kinases - metabolism | Molecular Structure | Protein Structure, Tertiary | Proto-Oncogene Proteins c-abl - genetics | src-Family Kinases - antagonists & inhibitors | Models, Molecular | Imatinib Mesylate | Adenosine Triphosphate - analogs & derivatives | Pyridines - metabolism | Proto-Oncogene Proteins c-abl - metabolism | Benzamides | Mutation | Adenosine Triphosphate - chemistry | src-Family Kinases - genetics | Protein Kinase Inhibitors - metabolism | Protein-Tyrosine Kinases - antagonists & inhibitors | Chemotherapy | Research | Protein kinases | Leukemia | Cancer | Enzymes | Molecular structure | Biological Sciences
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 06/2010, Volume 53, Issue 12, pp. 4701 - 4719
Journal Article
Journal Article
Blood, ISSN 0006-4971, 10/2004, Volume 104, Issue 8, pp. 2532 - 2539
The deregulated, oncogenic tyrosine kinase Bcr-Abl causes chronic myelold leukemia (CML). Imatinib mesylate (Gleevec, STI571), a Bcr-Abl kinase inhibitor,... 
CHRONIC MYELOGENOUS LEUKEMIA | GASTROINTESTINAL STROMAL TUMOR | STRUCTURAL BASIS | TYROSINE KINASE | PHILADELPHIA-CHROMOSOME | ACUTE LYMPHOBLASTIC-LEUKEMIA | CLINICAL RESISTANCE | HEMATOLOGY | IMATINIB MESYLATE | CHRONIC MYELOID-LEUKEMIA | STAT5 ACTIVATION | Apoptosis - drug effects | Humans | Gene Expression Regulation, Neoplastic | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - genetics | Piperazines - chemistry | Amino Acids - genetics | Pyrimidines - chemistry | Phosphotyrosine - metabolism | Adenosine Triphosphate - pharmacology | DNA-Binding Proteins - metabolism | Amino Acids - metabolism | Enzyme Inhibitors - chemistry | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - pathology | Inhibitory Concentration 50 | Phosphorylation - drug effects | Fusion Proteins, bcr-abl - chemistry | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology | Milk Proteins - metabolism | Protein Structure, Tertiary | Enzyme Inhibitors - pharmacology | Models, Molecular | Nuclear Proteins - metabolism | Pyrimidines - pharmacology | Mutation - genetics | Imatinib Mesylate | Piperazines - pharmacology | Adenosine Triphosphate - analogs & derivatives | Cell Division - drug effects | Fusion Proteins, bcr-abl - genetics | STAT5 Transcription Factor | Fusion Proteins, bcr-abl - antagonists & inhibitors | K562 Cells | HL-60 Cells | Trans-Activators - metabolism | Benzamides | Pyridones - chemistry | Adaptor Proteins, Signal Transducing - metabolism | Adenosine Triphosphate - chemistry | Cell Cycle - drug effects | Fusion Proteins, bcr-abl - metabolism | Pyridones - pharmacology
Journal Article
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2011, Volume 21, Issue 12, pp. 3743 - 3748
Journal Article
Journal Article
Chemical Biology & Drug Design, ISSN 1747-0277, 01/2006, Volume 67, Issue 1, pp. 46 - 57
The tyrosine kinase pp60src (Src) is the prototypical member of a family of proteins that participate in a broad array of cellular signal transduction... 
CYCLIN-DEPENDENT KINASES | ACTIVATION | COMPLEX | PHOSPHORYLATION | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | DRUG DISCOVERY | FAMILY KINASES | TARGETS | IDENTIFICATION | C-SRC | Catalytic Domain - drug effects | Humans | Protein Conformation - drug effects | Organophosphonates - metabolism | Substrate Specificity | Structure-Activity Relationship | Adenine - chemistry | Carbon - chemistry | Pyrimidines - chemistry | Adenosine Triphosphate - pharmacology | Adenosine Triphosphate - metabolism | Bone and Bones - metabolism | Enzyme Inhibitors - chemistry | Drug Design | Lymphocyte Specific Protein Tyrosine Kinase p56(lck) - chemistry | Purines - chemical synthesis | Adenine - analogs & derivatives | Enzyme Inhibitors - metabolism | Purines - pharmacology | src-Family Kinases - antagonists & inhibitors | Enzyme Inhibitors - pharmacology | Models, Molecular | Adenine - pharmacology | Cyclin-Dependent Kinase 2 - chemistry | Adenosine Triphosphate - analogs & derivatives | Neoplasms - drug therapy | Lymphocyte Specific Protein Tyrosine Kinase p56(lck) - antagonists & inhibitors | Organophosphonates - pharmacology | Purines - chemistry | Nitrogen - chemistry | Organophosphonates - chemistry | Cyclin-Dependent Kinase 2 - antagonists & inhibitors | Ligands | Adenine - metabolism | Adenosine Triphosphate - chemistry | src-Family Kinases - chemistry
Journal Article
Synthetic Communications, ISSN 0039-7911, 02/2007, Volume 37, Issue 3, pp. 417 - 423
The hydrogenation of iminonitriles and iminobisnitriles of type 1a-f is a particularly difficult process as the intermediate dieneamines are highly susceptible... 
triamine | hydrogenation | imino-bisnitrile | Triamine | Hydrogenation | Imino-bisnitrile | NMR | LIGANDS | ANALOGS | SAR | CHEMISTRY, ORGANIC | INHIBITORS | PROTEINS | DERIVATIVES
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 2007, Volume 48, Issue 41, pp. 7388 - 7391
The first example of a Heck reaction with 9-vinylpurines and aryl halides is described. It gives exclusively -9-(arenethenyl)purines in high yields. Subsequent... 
9-Vinylpurine | Heck reaction | 9-(Arenethyl)purine | 9-(Arenethenyl)purine | CROSS-COUPLING REACTIONS | DESIGN | PURINES | ANALOGS | ALKYLATION | KINASE | ARYLATION | CHLORIDES | CHEMISTRY, ORGANIC | INHIBITORS | DERIVATIVES | Substitution reactions | Purines
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 10/2006, Volume 12, Issue 20, pp. 6291s - 6295s
Src tyrosine kinase was the first gene product shown to have an essential function in bone using recombinant DNA technology after its expression was knocked... 
Journal Article
Annals of the New York Academy of Sciences, ISSN 0077-8923, 04/2006, Volume 1068, pp. 447 - 457
Understanding of the regulation of bone catabolism has advanced significantly over the past two decades with the identification of key enzymes that regulate... 
Journal Article
Bioorganic and Medicinal Chemistry, ISSN 0968-0896, 09/2008, Volume 18, Issue 17, pp. 4907 - 4912
Novel N super(9)-arenethenyl purines, optimized potent dual Src/Abl tyrosine kinase inhibitors, are described. The key structural feature is a trans vinyl... 
Journal Article