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Cancer Research, ISSN 0008-5472, 10/2004, Volume 64, Issue 19, pp. 7099 - 7109
Journal Article
Cancer Discovery, ISSN 2159-8274, 04/2017, Volume 7, Issue 4, pp. 400 - 409
Entrectinib, a potent oral inhibitor of the tyrosine kinases TRKA/B/C, ROS1, and ALK, was evaluated in two phase I studies in patients with advanced or... 
REARRANGEMENT | ONCOGENE | ONCOLOGY | ANALOG SECRETORY CARCINOMA | LANDSCAPE | KINASE FUSIONS | SARCOMAS | ETV6-NTRK3 GENE FUSION | CRIZOTINIB | GENOMIC ALTERATIONS | CLINICAL-RESPONSE | Benzamides - pharmacokinetics | Colorectal Neoplasms - genetics | Humans | Middle Aged | Receptor, trkA - antagonists & inhibitors | Male | Receptor, trkB - genetics | Indazoles - administration & dosage | Protein Kinase Inhibitors - adverse effects | Mammary Analogue Secretory Carcinoma - genetics | Dose-Response Relationship, Drug | Benzamides - administration & dosage | Membrane Glycoproteins - antagonists & inhibitors | Receptor, trkC - genetics | Anaplastic Lymphoma Kinase | Melanoma - genetics | Colorectal Neoplasms - drug therapy | Receptor, trkB - antagonists & inhibitors | Aged, 80 and over | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Adult | Female | Benzamides - adverse effects | Carcinoma, Non-Small-Cell Lung - pathology | Crizotinib | Protein Kinase Inhibitors - pharmacokinetics | Proto-Oncogene Proteins - antagonists & inhibitors | Pyridines - administration & dosage | Carcinoma, Non-Small-Cell Lung - genetics | Receptor, trkC - antagonists & inhibitors | Melanoma - pathology | Mammary Analogue Secretory Carcinoma - drug therapy | Membrane Glycoproteins - genetics | Protein Kinase Inhibitors - administration & dosage | Sequestosome-1 Protein - genetics | Pyrazoles - administration & dosage | Indazoles - pharmacokinetics | Receptor Protein-Tyrosine Kinases - genetics | Oncogene Proteins, Fusion - genetics | Melanoma - drug therapy | Adolescent | Receptor, trkA - genetics | Oncogene Proteins, Fusion - antagonists & inhibitors | Aged | Carcinoma, Non-Small-Cell Lung - drug therapy | Indazoles - adverse effects | Colorectal Neoplasms - pathology | Protein-Tyrosine Kinases - antagonists & inhibitors | Index Medicus
Journal Article
Journal of Hepatology, ISSN 0168-8278, 2011, Volume 55, Issue 3, pp. 612 - 625
Journal Article
Cancer Cell, ISSN 1535-6108, 2010, Volume 17, Issue 6, pp. 547 - 559
In mice, deletion and activation of results in lung tumors with a high penetrance of lymph node and distant metastases. We analyzed these primary and... 
CELLCYCLE | SIGNALING | EPITHELIAL-MESENCHYMAL TRANSITION | ONCOGENIC K-RAS | CANCER-CELLS | SUPPRESSOR | GENE | ONCOLOGY | SRC | KINASE INHIBITOR | EXPRESSION PROFILES | MUTATIONS | TUMORIGENESIS | Lung Neoplasms - drug therapy | Protein-Serine-Threonine Kinases - deficiency | Protein-Tyrosine Kinases - metabolism | Proto-Oncogene Proteins p21(ras) - genetics | Genomics | Humans | Lung Neoplasms - metabolism | Gene Expression Profiling | Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Cell Movement - genetics | Phosphorylation - genetics | RNA Interference | Gene Expression Regulation, Neoplastic - genetics | MAP Kinase Kinase 1 - antagonists & inhibitors | Carcinoma, Non-Small-Cell Lung - metabolism | Signal Transduction - genetics | Enzyme Inhibitors - therapeutic use | Focal Adhesion Protein-Tyrosine Kinases - antagonists & inhibitors | Focal Adhesion Protein-Tyrosine Kinases - genetics | Focal Adhesions - genetics | Signal Transduction - drug effects | Mice, Nude | Cell Line, Tumor | Mice | TOR Serine-Threonine Kinases | src-Family Kinases - genetics | Protein-Tyrosine Kinases - antagonists & inhibitors | ras Proteins - genetics | Lung Neoplasms - pathology | Cell Transdifferentiation - genetics | Protein-Tyrosine Kinases - genetics | Neoplasm Metastasis - drug therapy | Mice, Mutant Strains | Protein-Serine-Threonine Kinases - antagonists & inhibitors | src-Family Kinases - metabolism | Female | Drug Therapy, Combination | Lung Neoplasms - genetics | Cell Adhesion - genetics | Carcinoma, Non-Small-Cell Lung - genetics | Focal Adhesion Protein-Tyrosine Kinases - metabolism | Intracellular Signaling Peptides and Proteins - antagonists & inhibitors | src-Family Kinases - antagonists & inhibitors | Protein-Serine-Threonine Kinases - genetics | Proto-Oncogene Proteins - genetics | Up-Regulation - genetics | Xenograft Model Antitumor Assays | Neoplasm Metastasis - genetics | Animals | MAP Kinase Kinase 2 - antagonists & inhibitors | Protein Kinase Inhibitors - therapeutic use | Focal Adhesions - metabolism | Proteomics | Protein Kinase Inhibitors - pharmacology | Oncology, Experimental | Analysis | Lung cancer | Development and progression | Metastasis | Research | Cancer | Index Medicus
Journal Article
Molecular Biology of the Cell, ISSN 1059-1524, 04/2011, Volume 22, Issue 8, pp. 1191 - 1206
Mitosis requires precise coordination of multiple global reorganizations of the nucleus and cytoplasm. Cyclin-dependent kinase 1 (Cdk1) is the primary upstream... 
ANAPHASE-PROMOTING COMPLEX | XENOPUS EGG EXTRACTS | PROTEIN PHOSPHATASES | CYCLE-DEPENDENT PHOSPHORYLATION | UBIQUITIN LIGASE | M-PHASE | CHROMOSOME ALIGNMENT | CELL-CYCLE | TUMOR-CELLS | SPINDLE-ASSEMBLY CHECKPOINT | CELL BIOLOGY | Cyclin-Dependent Kinases - metabolism | Gene Expression - drug effects | Xenopus Proteins - genetics | Mitosis | Protein-Tyrosine Kinases - metabolism | Humans | Phosphoprotein Phosphatases - metabolism | G2 Phase - drug effects | CDC2 Protein Kinase - metabolism | Cell Cycle Proteins - antagonists & inhibitors | Protein-Tyrosine Kinases - genetics | Cyclin B - genetics | cdc25 Phosphatases - antagonists & inhibitors | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Cell Cycle Proteins - genetics | Prometaphase - drug effects | Female | Cyclin-Dependent Kinases - antagonists & inhibitors | Phosphorylation - drug effects | cdc25 Phosphatases - metabolism | Cyclin-Dependent Kinases - genetics | Nuclear Proteins - genetics | Protein-Serine-Threonine Kinases - metabolism | CDC2 Protein Kinase - genetics | Protein Phosphatase 2 - antagonists & inhibitors | CDC2 Protein Kinase - antagonists & inhibitors | Xenopus laevis | Cell Cycle Proteins - metabolism | Protein Phosphatase 2 - genetics | Protein-Serine-Threonine Kinases - genetics | Nuclear Proteins - metabolism | Phosphoprotein Phosphatases - antagonists & inhibitors | cdc25 Phosphatases - genetics | Xenopus Proteins - antagonists & inhibitors | Membrane Proteins | Animals | Phosphoprotein Phosphatases - genetics | Nuclear Proteins - antagonists & inhibitors | Protein Phosphatase 2 - metabolism | Cyclin B - metabolism | Feedback, Physiological - drug effects | Xenopus Proteins - metabolism | Protein Kinase Inhibitors - pharmacology | S Phase - drug effects | HeLa Cells | Protein-Tyrosine Kinases - antagonists & inhibitors | Index Medicus
Journal Article
Biochemical Journal, ISSN 0264-6021, 04/2013, Volume 451, Issue 2, pp. 313 - 328
Journal Article
Blood, ISSN 0006-4971, 12/2007, Volume 110, Issue 12, pp. 4055 - 4063
The BCR-ABL tyrosine kinase inhibitor imatinib represents the current frontline therapy in chronic myeloid leukemia. Because many patients develop imatinib... 
CHRONIC MYELOGENOUS LEUKEMIA | SELECTIVE INHIBITOR | DISCOIDIN DOMAIN RECEPTOR-1 | TYROSINE KINASE | PROTEIN-KINASE | CRYSTAL-STRUCTURE | DRUG DISCOVERY | INTRACELLULAR TARGETS | AFFINITY-CHROMATOGRAPHY | HEMATOLOGY | CHRONIC MYELOID-LEUKEMIA | Protein-Tyrosine Kinases - metabolism | Humans | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Drug Resistance, Neoplasm | Neoplasm Proteins - antagonists & inhibitors | Piperazines - chemistry | Thiazoles - therapeutic use | Neoplasm Proteins - metabolism | Pyrimidines - chemistry | Dose-Response Relationship, Drug | Protein Kinase Inhibitors - chemistry | Fusion Proteins, bcr-abl | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Protein-Serine-Threonine Kinases - metabolism | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology | Dasatinib | Quinone Reductases - metabolism | Piperazines - therapeutic use | Discoidin Domain Receptor 1 | Pyrimidines - pharmacology | Receptor Protein-Tyrosine Kinases - metabolism | Imatinib Mesylate | Piperazines - pharmacology | Protein Kinase Inhibitors - therapeutic use | Pyrimidines - therapeutic use | Quinone Reductases - antagonists & inhibitors | K562 Cells | Proteomics | Thiazoles - chemistry | Protein Kinase Inhibitors - pharmacology | Thiazoles - pharmacology | Benzamides | Drug Screening Assays, Antitumor | Protein-Tyrosine Kinases - antagonists & inhibitors | Index Medicus | Abridged Index Medicus
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2016, Volume 59, Issue 7, pp. 3392 - 3408
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase responsible for the development of different tumor types. Despite the remarkable clinical... 
CELL LUNG-CANCER | EML4-ALK | CHEMISTRY, MEDICINAL | FUSION | GENE | RESISTANCE | NEUROBLASTOMA | GENERATION | IDENTIFICATION | REARRANGEMENTS | ACTIVATING MUTATIONS | Lung Neoplasms - drug therapy | Rats, Wistar | Humans | Lung Neoplasms - metabolism | Receptor, trkA - antagonists & inhibitors | Crystallography, X-Ray | Lung Neoplasms - pathology | Antineoplastic Agents - administration & dosage | Indazoles - administration & dosage | Benzamides - administration & dosage | Protein Kinase Inhibitors - chemistry | Microsomes, Liver - drug effects | Receptor, trkB - antagonists & inhibitors | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Benzamides - pharmacology | Tumor Cells, Cultured | Benzamides - chemistry | Proto-Oncogene Proteins - antagonists & inhibitors | Indazoles - chemistry | Administration, Oral | Crystallization | Receptor, trkC - antagonists & inhibitors | Rats | Antineoplastic Agents - chemistry | Mice, SCID | Blood-Brain Barrier - drug effects | Drug Discovery | Blotting, Western | Indazoles - pharmacology | Xenograft Model Antitumor Assays | Protein Kinase Inhibitors - administration & dosage | Animals | Mice, Nude | Cell Membrane Permeability - drug effects | Dogs | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Protein-Tyrosine Kinases - antagonists & inhibitors | Index Medicus
Journal Article
The New England Journal of Medicine, ISSN 0028-4793, 08/2017, Volume 377, Issue 9, pp. 829 - 838
Alectinib, a potent ALK tyrosine kinase inhibitor, was more effective and somewhat less toxic than crizotinib when used as primary therapy in patients with ALK... 
RESISTANT | MEDICINE, GENERAL & INTERNAL | MODELS | ANTITUMOR-ACTIVITY | INHIBITOR ALECTINIB | CHEMOTHERAPY | Lung Neoplasms - drug therapy | Pyrazoles - therapeutic use | Follow-Up Studies | Lung Neoplasms - mortality | Humans | Middle Aged | Male | Antineoplastic Agents - therapeutic use | Protein Kinase Inhibitors - adverse effects | Central Nervous System Neoplasms - secondary | Young Adult | Pyridines - adverse effects | Anaplastic Lymphoma Kinase | Antineoplastic Agents - adverse effects | Aged, 80 and over | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Adult | Female | Receptor Protein-Tyrosine Kinases - analysis | Pyrazoles - adverse effects | Pyridines - therapeutic use | Crizotinib | Carbazoles - adverse effects | Kaplan-Meier Estimate | Carcinoma, Non-Small-Cell Lung - mortality | Disease-Free Survival | Animals | Piperidines - therapeutic use | Protein Kinase Inhibitors - therapeutic use | Piperidines - adverse effects | Intention to Treat Analysis | Carbazoles - therapeutic use | Carcinoma, Non-Small-Cell Lung - drug therapy | Central Nervous System Neoplasms - drug therapy | Drugs | Care and treatment | Analysis | Comparative analysis | Lung cancer, Non-small cell | Health aspects | Systemic diseases | Toxicity | Lung cancer | Central nervous system | Oncology | Nervous system | Metastasis | Radiation therapy | Patients | Lymphoma | Cancer therapies | Survival | Mutation | Protein-tyrosine kinase | Drug dosages | Tumors | Index Medicus | Abridged Index Medicus
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2011, Volume 54, Issue 18, pp. 6342 - 6363
Journal Article
Science, ISSN 0036-8075, 12/2014, Volume 346, Issue 6216, pp. 1480 - 1486
Targeted cancer therapies have produced substantial clinical responses, but most tumors develop resistance to these drugs. Here, we describe a pharmacogenomic... 
CELL LUNG-CANCER | ALK | KINASE INHIBITION | GEFITINIB | ACTIVATION | CERITINIB | MULTIDISCIPLINARY SCIENCES | CRIZOTINIB | MUTATIONS | CHEMOTHERAPY | BYPASS MECHANISMS | Lung Neoplasms - drug therapy | Sulfones - therapeutic use | Humans | Receptor, Fibroblast Growth Factor, Type 3 - antagonists & inhibitors | MAP Kinase Kinase 1 - genetics | DNA Mutational Analysis | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Tumor Cells, Cultured | Molecular Targeted Therapy - methods | Lung Neoplasms - genetics | Receptor, Fibroblast Growth Factor, Type 3 - genetics | Lung Neoplasms - enzymology | Carcinoma, Non-Small-Cell Lung - genetics | MAP Kinase Kinase 1 - metabolism | Proto-Oncogene Proteins pp60(c-src) - antagonists & inhibitors | Patient-Specific Modeling | Drug Resistance, Neoplasm - genetics | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Protein Kinase Inhibitors - therapeutic use | Pyrimidines - therapeutic use | Receptor, Epidermal Growth Factor - antagonists & inhibitors | Carcinoma, Non-Small-Cell Lung - drug therapy | Carcinoma, Non-Small-Cell Lung - enzymology | Mutation | Enzyme Activation - genetics | Drug Screening Assays, Antitumor | Antimitotic agents | Cancer patients | Care and treatment | Lung cancer | Dosage and administration | Genetic aspects | Antineoplastic agents | Drug therapy | Drug resistance | Methods | Cancer | Cell culture | Oncology | Pharmaceutical sciences | Index Medicus | Drugs | Mutations | Therapy | Genetics | Kinases | Patients | Tumors
Journal Article