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Cancer discovery, ISSN 2159-8290, 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
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
The New England journal of medicine, ISSN 1533-4406, 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
Biology of Blood and Marrow Transplantation, ISSN 1083-8791, 2013, Volume 19, Issue 1, pp. 150 - 155
Journal Article
The Journal of clinical investigation, ISSN 0021-9738, 2012, Volume 122, Issue 4, pp. 1377 - 1392
Journal Article
Pulmonary Pharmacology & Therapeutics, ISSN 1094-5539, 2010, Volume 23, Issue 4, pp. 235 - 256
Abstract After more than two decades of research into phosphodiesterase 4 (PDE4) inhibitors, roflumilast... 
Medical Education | Pulmonary/Respiratory | Phosphodiesterase 4 | Inflammation | Roflumilast | Oral therapy | COPD | Preclinical pharmacology | SMOKE-INDUCED EMPHYSEMA | OXIDATIVE STRESS | FIBROBLAST-MEDIATED CONTRACTION | NECROSIS-FACTOR-ALPHA | ADHESION MOLECULES | PDE4 INHIBITORS | TRANSMEMBRANE CONDUCTANCE REGULATOR | RESPIRATORY SYSTEM | EPIDERMAL-GROWTH-FACTOR | PHARMACOLOGY & PHARMACY | ENDOTHELIAL CELL-INTERACTIONS | CIGARETTE-SMOKE | Phosphodiesterase Inhibitors - therapeutic use | Phosphodiesterase Inhibitors - adverse effects | Administration, Oral | Humans | Aminopyridines - adverse effects | Phosphodiesterase Inhibitors - pharmacology | Pulmonary Disease, Chronic Obstructive - physiopathology | Cyclopropanes - adverse effects | Inflammation - etiology | Anti-Inflammatory Agents, Non-Steroidal - pharmacology | Cyclopropanes - therapeutic use | Animals | Anti-Inflammatory Agents, Non-Steroidal - adverse effects | Benzamides - therapeutic use | Aminopyridines - therapeutic use | Anti-Inflammatory Agents, Non-Steroidal - therapeutic use | Inflammation - drug therapy | Aminopyridines - pharmacology | Phosphodiesterase 4 Inhibitors | Benzamides - pharmacology | Drug Evaluation, Preclinical | Benzamides - adverse effects | Cyclopropanes - pharmacology | Pulmonary Disease, Chronic Obstructive - drug therapy | Lung diseases, Obstructive | Isoenzymes | Comorbidity | Respiratory agents | Pharmacology | T cells | Macrophages | Pulmonary hypertension | Endothelium | Metabolites | Universities and colleges | Smoking
Journal Article
Nature (London), ISSN 1476-4687, 2017, Volume 546, Issue 7657, pp. 259 - 264
The human glucagon receptor, GCGR, belongs to the class B G-protein-coupled receptor family and plays a key role in glucose homeostasis and the pathophysiology... 
Medicine(all) | General | REFINEMENT | EXTRACELLULAR DOMAINS | LIPIDIC CUBIC PHASE | CORTICOTROPIN-RELEASING-FACTOR | MULTIDISCIPLINARY SCIENCES | DRUG DISCOVERY | VALIDATION | BINDING-SITE | SERIAL FEMTOSECOND CRYSTALLOGRAPHY | LIGAND | SOFTWARE | Receptors, Glucagon - agonists | Cross-Linking Reagents - chemistry | Allosteric Site - drug effects | Humans | Benzamides - metabolism | Models, Molecular | Receptors, Glucagon - metabolism | Crystallography, X-Ray | Receptors, Glucagon - classification | Molecular Dynamics Simulation | Deuterium Exchange Measurement | Disulfides - chemistry | Phenylurea Compounds - chemistry | Receptors, Glucagon - chemistry | Protein Domains | Ligands | Benzamides - pharmacology | Cell Membrane - metabolism | Phenylurea Compounds - metabolism | Phenylurea Compounds - pharmacology | Protein Stability | Benzamides - chemistry | Protein structure prediction | G proteins | Glucagon | Structure | Health aspects | Methods | Deuterium | Dynamic structural analysis | Exchanging | G protein-coupled receptors | Molecular structure | Hydrogen | Hydrogen-deuterium exchange | Diabetes mellitus | Homeostasis | Molecular dynamics | Crosslinking | Forming | Activation | Glucose | Guanine nucleotide-binding protein | Coupling (molecular) | Proteins | Signaling | Receptors | Receptor mechanisms | Diabetes | Protein structure | Crystal structure
Journal Article