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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
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 09/2017, Volume 23, Issue 18, pp. 5366 - 5373
Purpose: Squamous cell lung cancers (SQCLC) account for 25% of all NSCLCs, yet the prognosis of these patients is poor and treatment options are limited.... 
ACTIVATION | ONCOLOGY | THERAPEUTIC TARGET | FGFR1 | Piperazines - administration & dosage | Lung Neoplasms - drug therapy | Pyrazoles - therapeutic use | Benzamides - pharmacokinetics | Carcinoma, Squamous Cell - genetics | Carcinoma, Squamous Cell - pathology | Humans | Middle Aged | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Lung Neoplasms - pathology | Male | Antineoplastic Agents - therapeutic use | Gene Expression Profiling | Antineoplastic Agents - administration & dosage | Receptor, Fibroblast Growth Factor, Type 1 - genetics | Benzamides - administration & dosage | Neoplasm Metastasis | Benzamides - therapeutic use | Neoplasm Grading | Antineoplastic Agents - adverse effects | Female | Antineoplastic Agents - pharmacokinetics | Piperazines - pharmacokinetics | Pyrazoles - pharmacokinetics | Benzamides - adverse effects | Pyrazoles - adverse effects | Lung Neoplasms - genetics | Treatment Outcome | Chromosomes, Human, Pair 8 | Piperazines - therapeutic use | Piperazines - adverse effects | Sequence Analysis, DNA | Genetic Heterogeneity | Pyrazoles - administration & dosage | Carcinoma, Squamous Cell - drug therapy | Gene Amplification | Aged | Neoplasm Staging | Immunohistochemistry | Pharmacodynamics | Lung cancer | Pharmacology | Gene expression | Patients | Gene sequencing | Anticancer properties | Amplification | Gene amplification | Experimental design | Safety engineering | Medical prognosis | Cell lines | Chromosome 8 | Xenografts | Antitumor activity | Pharmacokinetics | Fibroblast growth factor receptor 1 | Tumors | Cancer | Fibroblast growth factor receptors
Journal Article
Journal Article
Nature, ISSN 0028-0836, 09/2015, Volume 525, Issue 7569, pp. 380 - 383
Whether cancer is maintained by a small number of stem cells or is composed of proliferating cells with approximate phenotypic equivalency is a central... 
CANCER-CELLS | MAINTENANCE | ACTIVATION | HEMATOPOIESIS | PATHWAY | CITED2 | MULTIDISCIPLINARY SCIENCES | IMATINIB | STAT5 | DIFFERENTIATION | HIF-1-ALPHA | Piperazines - administration & dosage | Antineoplastic Combined Chemotherapy Protocols - administration & dosage | Cell Proliferation | Neoplastic Stem Cells - drug effects | Humans | Gene Expression Regulation, Neoplastic | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - genetics | PPAR gamma - metabolism | Thiazolidinediones - administration & dosage | Antineoplastic Combined Chemotherapy Protocols - pharmacology | STAT5 Transcription Factor - metabolism | Benzamides - administration & dosage | Thiazolidinediones - therapeutic use | Benzamides - therapeutic use | Basic Helix-Loop-Helix Transcription Factors - metabolism | Neoplastic Stem Cells - metabolism | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - pathology | Neoplastic Stem Cells - pathology | Benzamides - pharmacology | Thiazolidinediones - pharmacology | Repressor Proteins - metabolism | Pyrimidines - administration & dosage | Piperazines - therapeutic use | Pyrimidines - pharmacology | Imatinib Mesylate | Piperazines - pharmacology | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Pyrimidines - therapeutic use | PPAR gamma - agonists | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - metabolism | Trans-Activators - metabolism | Life Sciences | Microbiology and Parasitology | Immunology | Bacteriology | Virology
Journal Article
Journal of Clinical Investigation, ISSN 0021-9738, 12/2011, Volume 121, Issue 12, pp. 4700 - 4711
Advanced human thyroid cancers, particularly those that are refractory to treatment with radioiodine (RAI), have a high prevalence of BRAF (v-raf murine... 
MEDICINE, RESEARCH & EXPERIMENTAL | GROWTH-INHIBITION | BRAF(V600E) MUTATION | CARCINOMA CELLS | GENE | RAS | ANTISENSE RNA | KINASE | SENSITIVITY | PROLIFERATION | EXPRESSION | MAP Kinase Signaling System - physiology | Proto-Oncogene Proteins B-raf - physiology | Apoptosis - drug effects | Humans | Antineoplastic Agents - therapeutic use | Mutation, Missense | Indoles - administration & dosage | Benzamides - administration & dosage | Neoplasm Proteins - genetics | MAP Kinase Kinase 1 - antagonists & inhibitors | Benzamides - toxicity | Diphenylamine - therapeutic use | Carcinoma, Papillary - drug therapy | Mice, Transgenic | Diphenylamine - toxicity | Sulfonamides - pharmacology | Antineoplastic Combined Chemotherapy Protocols - toxicity | Protein Kinase Inhibitors - administration & dosage | Indoles - therapeutic use | Mice | DNA Damage | Thyroid Gland - metabolism | Sulfonamides - administration & dosage | Thyroid Neoplasms - metabolism | Carcinoma, Papillary - genetics | Diphenylamine - pharmacology | Neoplasm Proteins - physiology | Carcinoma, Papillary - metabolism | Diphenylamine - analogs & derivatives | Benzamides - therapeutic use | Indoles - pharmacology | Benzamides - pharmacology | Diphenylamine - administration & dosage | Genes, Synthetic - drug effects | Indoles - toxicity | Enzyme Activation - drug effects | Iodine Radioisotopes - pharmacokinetics | Carcinoma, Papillary - pathology | Point Mutation | Thyroid Neoplasms - genetics | Animals | MAP Kinase Signaling System - drug effects | Sulfonamides - therapeutic use | Thyroid Neoplasms - drug therapy | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Protein Kinase Inhibitors - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Protein Kinase Inhibitors - toxicity | Sulfonamides - toxicity | Protein Kinase Inhibitors - pharmacology | Doxorubicin - pharmacology | Drug Screening Assays, Antitumor | Thyroid Neoplasms - pathology | Care and treatment | Thyroid cancer | Cancer cells | Genetic aspects | Diagnosis | Properties | Isotopes | Health aspects | Mitogen-activated protein kinases | Iodine
Journal Article
Science, ISSN 0036-8075, 9/2011, Volume 333, Issue 6047, pp. 1292 - 1296
Ionic flux mediates essential physiological and behavioral functions in defined cell populations. Cell type—specific activators of diverse ionic conductances... 
Brain | Receptors | Neurons | Drug interactions | REPORTS | Ligands | Ion channels | Pharmacology | Benzamides | Cholinergic receptors | Behavioral neuroscience | ACETYLCHOLINE-RECEPTORS | DESIGN | DOMAIN | PROTEIN | NEURONAL NICOTINIC RECEPTOR | DESENSITIZATION | MULTIDISCIPLINARY SCIENCES | IN-VIVO | LOOP | MUTATIONS | IDENTIFICATION | Stereoisomerism | Humans | Benzamides - metabolism | Brain - physiology | Recombinant Fusion Proteins - metabolism | Bridged Bicyclo Compounds - chemistry | Receptors, Nicotinic - chemistry | HEK293 Cells | Neurons - physiology | Protein Engineering | Female | Benzamides - pharmacology | Receptors, Glycine - metabolism | Ligand-Gated Ion Channels - metabolism | Benzamides - chemistry | Protein Structure, Tertiary | Brain - cytology | Receptors, Nicotinic - metabolism | Receptors, Serotonin, 5-HT3 - genetics | Bridged Bicyclo Compounds - pharmacology | Ligand-Gated Ion Channels - chemistry | Mice, Inbred C57BL | Quinuclidines - pharmacology | Feeding Behavior | Recombinant Fusion Proteins - chemistry | Patch-Clamp Techniques | Animals | Membrane Potentials | Mutagenesis | Small Molecule Libraries | Bridged Bicyclo Compounds - metabolism | Ligand-Gated Ion Channels - genetics | Receptors, Serotonin, 5-HT3 - metabolism | Protein Binding | Mice | Quinuclidines - chemistry | Ion Channel Gating | Quinuclidines - metabolism | Receptors, Glycine - genetics | Receptors, Nicotinic - genetics | alpha7 Nicotinic Acetylcholine Receptor | Physiological aspects | Usage | Genetic engineering | Research | Animal behavior | Ligands (Biochemistry) | Ions | Cellular biology | Chemical engineering
Journal Article
The New England Journal of Medicine, ISSN 0028-4793, 01/2016, Volume 374, Issue 4, pp. 323 - 332
Acalabrutinib is an irreversible inhibitor of Bruton's tyrosine kinase with greater specificity for the enzyme than the first-in-class agent, ibrutinib. It had... 
B-CELL RECEPTOR | MEDICINE, GENERAL & INTERNAL | ACTIVATION | IN-VIVO | X-LINKED AGAMMAGLOBULINEMIA | IBRUTINIB | BTK | PCI-32765 | TYROSINE KINASE INHIBITOR | LYMPHOMA | OPEN-LABEL | Recurrence | Benzamides - pharmacokinetics | Humans | Middle Aged | Pyrazines - administration & dosage | Male | Antineoplastic Agents - administration & dosage | Leukemia, Lymphocytic, Chronic, B-Cell - genetics | Protein Kinase Inhibitors - adverse effects | Diarrhea - chemically induced | Dose-Response Relationship, Drug | Benzamides - administration & dosage | Antineoplastic Agents - adverse effects | Female | Antineoplastic Agents - pharmacokinetics | Benzamides - adverse effects | Headache - chemically induced | Chromosome Deletion | Protein Kinase Inhibitors - pharmacokinetics | Administration, Oral | Disease-Free Survival | Protein Kinase Inhibitors - administration & dosage | Agammaglobulinaemia Tyrosine Kinase | Pyrazines - pharmacokinetics | Pyrazines - adverse effects | Aged | Leukemia, Lymphocytic, Chronic, B-Cell - drug therapy | Protein-Tyrosine Kinases - antagonists & inhibitors | Antimitotic agents | Treatment outcome | Usage | Care and treatment | Safety and security measures | Lymphocytic leukemia | Analysis | Clinical trials | Pharmacology | Dosage and administration | Pharmacokinetics | Antineoplastic agents | Tyrosine | Headache | Pharmacodynamics | Transformation | Chronic lymphatic leukemia | Inhibitor drugs | Leukemia | Diarrhea | Chromosome deletion | Lymphatic leukemia | Kinases | Lymphoma | Bruton's tyrosine kinase | Patients | Clonal deletion | Lymphomas | Safety | Drug therapy | Lymphocytosis | Protein-tyrosine kinase | Chromosome 17 | Index Medicus | Abridged Index Medicus
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2001, Volume 44, Issue 23, pp. 3764 - 3767
Journal Article
Journal Article
Biology of Blood and Marrow Transplantation, ISSN 1083-8791, 2013, Volume 19, Issue 1, pp. 150 - 155
Journal Article