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Science Signaling, ISSN 1945-0877, 11/2017, Volume 10, Issue 507, p. eaam7550
Activation of the RAS-RAF-MEK-ERK signaling pathway is implicated in driving the initiation and progression of multiple cancers. Several inhibitors targeting... 
RAS | BIOCHEMISTRY & MOLECULAR BIOLOGY | ALK MUTATIONS | AKT | LARGE-CELL LYMPHOMA | HIGH-RISK NEUROBLASTOMA | COMPLEX INTEGRITY | NEGATIVE FEEDBACK | MUTANT LUNG-CANCER | UP-REGULATION | ACTIVATING MUTATIONS | CELL BIOLOGY | Lung Neoplasms - drug therapy | Oncogene Proteins, Fusion - metabolism | Humans | Neuroblastoma - enzymology | Antineoplastic Agents - therapeutic use | Mitogen-Activated Protein Kinase 7 - antagonists & inhibitors | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Female | Pyrimidinones - pharmacology | Antineoplastic Agents - pharmacology | Mechanistic Target of Rapamycin Complex 2 - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - metabolism | Lung Neoplasms - enzymology | Pyrimidinones - therapeutic use | Mitogen-Activated Protein Kinase 7 - metabolism | Xenograft Model Antitumor Assays | Mechanistic Target of Rapamycin Complex 2 - metabolism | Animals | MAP Kinase Signaling System - drug effects | Receptor Protein-Tyrosine Kinases - genetics | Protein Kinase Inhibitors - therapeutic use | Neuroblastoma - drug therapy | Cell Line, Tumor | Oncogene Proteins, Fusion - antagonists & inhibitors | Mice | Mice, Inbred BALB C | Protein Kinase Inhibitors - pharmacology | Pyridones - therapeutic use | Proto-Oncogene Proteins c-akt - antagonists & inhibitors | Pyridones - pharmacology | TOR protein | Biotechnology | Phosphorylation | Xenotransplantation | Lung cancer | Raf protein | AKT protein | Activation | Neuroblastoma | Kinases | Neuroblastoma cells | Signal transduction | Feedback | Xenografts | Inhibition | Protein-tyrosine kinase | Epidermal growth factor receptors | Therapeutic applications | MEK inhibitors | Extracellular signal-regulated kinase | MAP kinase | Rapamycin | Ras protein | Patients | Lymphoma | Signaling | Inhibitors | Cell lines | Mutation | Cancer | Index Medicus | Cell and Molecular Biology | Cell- och molekylärbiologi
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 05/2013, Volume 19, Issue 10, pp. 2677 - 2687
Purpose: To analyze the antimyeloma potential of TG02, an ERK5/CDK inhibitory drug. Experimental Design: Utilizing different multiple myeloma cell lines we... 
MULTIPLE-MYELOMA | CANCER-CELLS | ACTIVATION | ONCOLOGY | INDUCED APOPTOSIS | CYCLIN D1 | PHOSPHORYLATION | SENSITIVITY | TRANSDUCTION | DEPENDENT KINASE INHIBITOR | EXPRESSION | Cell Cycle - genetics | Gene Expression Regulation, Enzymologic - drug effects | Cyclin-Dependent Kinases - metabolism | Humans | Cell Survival - genetics | Thalidomide - pharmacology | Heterocyclic Compounds, 4 or More Rings - pharmacology | CDC2 Protein Kinase - metabolism | Dose-Response Relationship, Drug | Thalidomide - analogs & derivatives | Mitogen-Activated Protein Kinase 7 - antagonists & inhibitors | Female | Cyclin-Dependent Kinases - antagonists & inhibitors | Gene Expression Regulation, Neoplastic - drug effects | Cyclin-Dependent Kinases - genetics | Multiple Myeloma - enzymology | Cell Survival - drug effects | Cyclin-Dependent Kinase 2 - metabolism | CDC2 Protein Kinase - genetics | Bortezomib | CDC2 Protein Kinase - antagonists & inhibitors | Cyclin-Dependent Kinase 9 - genetics | Cyclin-Dependent Kinase 2 - genetics | Cyclin-Dependent Kinase 9 - antagonists & inhibitors | Mitogen-Activated Protein Kinase 7 - genetics | Mitogen-Activated Protein Kinase 7 - metabolism | Mice, SCID | Reverse Transcriptase Polymerase Chain Reaction | Blotting, Western | Drug Synergism | Xenograft Model Antitumor Assays | Multiple Myeloma - pathology | Animals | Cell Line, Tumor | Cyclin-Dependent Kinase 2 - antagonists & inhibitors | Cyclin-Dependent Kinase 9 - metabolism | Protein Kinase Inhibitors - pharmacology | Multiple Myeloma - prevention & control | Cell Cycle - drug effects | Pyrazines - pharmacology | Boronic Acids - pharmacology | Index Medicus
Journal Article
Cancer Cell, ISSN 1535-6108, 2010, Volume 18, Issue 3, pp. 258 - 267
Journal Article
Biochemical and Biophysical Research Communications, ISSN 0006-291X, 2008, Volume 377, Issue 1, pp. 120 - 125
Journal Article
Cancer Letters, ISSN 0304-3835, 2016, Volume 381, Issue 2, pp. 314 - 322
Research Highlights • BIX02189 inhibits TGF-β1-induced EMT and cell migration in A549 lung cancer cells. • The inhibitory effect of BIX02189 is independent of... 
Hematology, Oncology and Palliative Medicine | TβRI | TGF-β1 | BIX02189 | EMT | Lung cancer | Lung Neoplasms - drug therapy | Aniline Compounds - metabolism | Humans | Lung Neoplasms - metabolism | Epithelial-Mesenchymal Transition - drug effects | Lung Neoplasms - pathology | Antineoplastic Agents - metabolism | Dose-Response Relationship, Drug | Indoles - metabolism | Carcinoma, Non-Small-Cell Lung - secondary | Transfection | RNA Interference | Adenosine Triphosphate - metabolism | MAP Kinase Kinase 5 - metabolism | Mitogen-Activated Protein Kinase 7 - antagonists & inhibitors | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Female | Indoles - pharmacology | Antineoplastic Agents - pharmacology | Binding Sites | Protein-Serine-Threonine Kinases - metabolism | Transforming Growth Factor beta1 - pharmacology | Lung Neoplasms - genetics | A549 Cells | Aniline Compounds - pharmacology | Carcinoma, Non-Small-Cell Lung - genetics | Neoplasm Invasiveness | Carcinoma, Non-Small-Cell Lung - metabolism | MAP Kinase Kinase 5 - antagonists & inhibitors | Mitogen-Activated Protein Kinase 7 - genetics | MAP Kinase Kinase 5 - genetics | Mitogen-Activated Protein Kinase 7 - metabolism | Xenograft Model Antitumor Assays | Cell Movement - drug effects | Animals | Receptors, Transforming Growth Factor beta - antagonists & inhibitors | Receptors, Transforming Growth Factor beta - metabolism | Signal Transduction - drug effects | Mice, Nude | Protein Binding | Mice, Inbred BALB C | Molecular Docking Simulation | Protein Kinase Inhibitors - pharmacology | Carcinoma, Non-Small-Cell Lung - drug therapy | Smad Proteins - metabolism | Index Medicus
Journal Article
PLoS ONE, ISSN 1932-6203, 09/2014, Volume 9, Issue 9, pp. e109047 - e109047
The fibroblast mitogen platelet-derived growth factor -BB (PDGF-BB) induces a transient expression of the orphan nuclear receptor NR4A1 (also named Nur77, TR3... 
APOPTOSIS | ACTIVATED PROTEIN-KINASE | NUCLEAR RECEPTORS | MULTIDISCIPLINARY SCIENCES | TRANSCRIPTION | NUR77 | ORPHAN RECEPTOR TR3 | GASTRIC-CANCER CELLS | NF-KAPPA-B | EXPRESSION | TERMINAL KINASE | NIH 3T3 Cells | RNA, Small Interfering - genetics | Nuclear Receptor Subfamily 4, Group A, Member 1 - antagonists & inhibitors | Nitriles - pharmacology | Neuroglia - pathology | Humans | NF-kappa B - metabolism | RNA, Messenger - metabolism | Sulfones - pharmacology | Neuroglia - drug effects | MAP Kinase Kinase 1 - genetics | Mitogen-Activated Protein Kinase 7 - antagonists & inhibitors | RNA, Messenger - antagonists & inhibitors | Benzamides - pharmacology | Proto-Oncogene Proteins c-sis - pharmacology | MAP Kinase Kinase 2 - genetics | Cell Survival - drug effects | MAP Kinase Kinase 1 - antagonists & inhibitors | NF-kappa B - antagonists & inhibitors | Nuclear Receptor Subfamily 4, Group A, Member 1 - genetics | Signal Transduction | RNA, Messenger - genetics | Gene Expression Regulation | Agar | MAP Kinase Kinase 1 - metabolism | Becaplermin | MAP Kinase Kinase 2 - metabolism | Mitogen-Activated Protein Kinase 7 - genetics | Chemotaxis - drug effects | Mitogen-Activated Protein Kinase 7 - metabolism | Animals | NF-kappa B - genetics | MAP Kinase Kinase 2 - antagonists & inhibitors | Cell Line, Tumor | Nuclear Receptor Subfamily 4, Group A, Member 1 - metabolism | Neuroglia - metabolism | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | RNA, Small Interfering - metabolism | RNA | Platelet-derived growth factor | Cell proliferation | Phosphorylation | Transcription factors | Glioblastoma | Nur77 protein | Smooth muscle | mRNA | Kinases | Nuclei | Cell adhesion & migration | Proteins | Signal transduction | Cell growth | Cell cycle | Tumorigenesis | Localization | Deoxyribonucleic acid--DNA | NF-κB protein | Medical research | Cell survival | Pulmonary arteries | Melanoma | Breast cancer | T cell receptors | Gene expression | Platelet-derived growth factor BB | Inhibitors | Pancreatic cancer | Medical prognosis | Cell lines | Ligands | Cytoplasm | Apoptosis | Index Medicus | Clinical Medicine | Medical and Health Sciences | Cancer and Oncology | Klinisk medicin | Medicin och hälsovetenskap | Cancer och onkologi | Deoxyribonucleic acid | DNA
Journal Article
Cellular Signalling, ISSN 0898-6568, 03/2016, Volume 28, Issue 3, pp. 177 - 189
Extracellular signal-regulated kinases (ERKs) play important roles in proliferation, differentiation and gene expression. In our previous study, we... 
Nerve growth factor (NGF) | Pheochromocytoma | Extracellular-signal regulated kinase (ERK) | Tyrosine hydroxylase (TH) | Sympathetic neurons | Ankyrin repeat domain 1 (ankrd1) | ACTIVATION | ANKYRIN REPEAT PROTEIN | TYROSINE-HYDROXYLASE | KINASE 5 | NERVE GROWTH-FACTOR | CELL BIOLOGY | NEURONAL SURVIVAL | GENE | SIGNALING PATHWAY | PC12 CELLS | TARGETED DELETION | Tyrosine 3-Monooxygenase - metabolism | Humans | Middle Aged | Mitogen-Activated Protein Kinase 3 - antagonists & inhibitors | Male | Chromatography, High Pressure Liquid | PC12 Cells | Repressor Proteins - antagonists & inhibitors | Tandem Mass Spectrometry | RNA Interference | Catecholamines - analysis | Mitogen-Activated Protein Kinase 7 - antagonists & inhibitors | Muscle Proteins - metabolism | Aged, 80 and over | Pheochromocytoma - pathology | Adult | Female | Muscle Proteins - antagonists & inhibitors | Nuclear Proteins - genetics | Adrenal Gland Neoplasms - pathology | Repressor Proteins - metabolism | Pheochromocytoma - metabolism | Mitogen-Activated Protein Kinase 1 - antagonists & inhibitors | Nerve Growth Factor - pharmacology | Rats | Repressor Proteins - genetics | Nuclear Proteins - metabolism | Mitogen-Activated Protein Kinase 7 - genetics | Mitogen-Activated Protein Kinase 7 - metabolism | Down-Regulation - drug effects | Muscle Proteins - genetics | Up-Regulation - drug effects | Animals | Mitogen-Activated Protein Kinase 3 - metabolism | Signal Transduction - drug effects | Nuclear Proteins - antagonists & inhibitors | Adolescent | Adrenal Gland Neoplasms - metabolism | Aged | Catecholamines - biosynthesis | Microscopy, Fluorescence | Mitogen-Activated Protein Kinase 1 - metabolism | RNA, Small Interfering - metabolism | Physiological aspects | Nerve growth factor | DNA microarrays | RNA | Analysis | Tyrosine | Epidermal growth factor | Neurons | Fibroblast growth factors | Hydroxylases | Gene expression | Index Medicus | International trade | Nerves | Biosynthesis | Kinases | Differentiation | Catecholamine | Growth factors | extracellular-signal regulated kinase (ERK) | pheochromocytoma | sympathetic neurons | tyrosine hydroxylase (TH) | ankyrin repeat domain 1 (ankrd1) | nerve growth factor (NGF)
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 12/2013, Volume 70, pp. 758 - 767
The benzo[ ]pyrimido-[5,4- ]diazepine-6(11 )-one core was discovered as a novel ERK5 (also known as MAPK7 and BMK1) inhibitor scaffold, previously. Further... 
ERK5 inhibitor | Benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-one | Kinase selectivity | Benzo[e]pyrimido-[5,4-b]diazepine-6(11H)- one | CELLS | CHEMISTRY, MEDICINAL | ACTIVATED PROTEIN-KINASE | INHIBITOR SELECTIVITY | POLO-LIKE-KINASE-1 | LRRK2 | PARKINSON DISEASE | PROSTATE-CANCER | IN-VIVO | EXPRESSION | CARCINOMA | Protein Kinase Inhibitors - chemical synthesis | Pyrimidines - chemical synthesis | Humans | Cells, Cultured | Azepines - chemical synthesis | Models, Molecular | Structure-Activity Relationship | Mitogen-Activated Protein Kinase 7 - metabolism | Pyrimidines - pharmacology | Enzyme Activation - drug effects | Pyrimidines - chemistry | Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 | Azepines - pharmacology | Dose-Response Relationship, Drug | Protein Kinase Inhibitors - chemistry | Azepines - chemistry | Mitogen-Activated Protein Kinase 7 - antagonists & inhibitors | HEK293 Cells | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Molecular Structure | Protein Kinase Inhibitors - pharmacology | HeLa Cells | Protein-Serine-Threonine Kinases - metabolism | Medical colleges | Phosphotransferases | Epidermal growth factor | Index Medicus | PLK, polo-like kinase | EGF, epidermal growth factor | PML, promyelocytic leukemia protein | X-phos, 2-dicyclohexylphosphino-2′,4′,6′-triisopropyl-biphenyl | DIEA, N,N-diisopropylethylamine | DMA, N,N-dimethylacetamide | ERK5, extracelluar-signal-regulated kinase 5 | LRRK2, leucine rich repeat kinase 2 | BMK1, big MAP kinase 1 | ERK5, mitogen-activated protein kinase 7 | RSK, ribosomal S6 kinase | SAR, structure–activity relationship | Pd2(dba)3, tris(dibenzylideneacetone)dipalladium- | HCC, hepatocellular carcinoma | Original | DCAMKL2, doublecortin and CaM kinase-like 2 | MAPK, mitogen-activated protein kinase | MEK5, MAP kinase kinase 5
Journal Article
Journal Article
Experimental Cell Research, ISSN 0014-4827, 01/2015, Volume 330, Issue 1, pp. 199 - 211
Journal Article