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Biochemical Journal, ISSN 0264-6021, 12/2007, Volume 408, Issue 3, pp. 297 - 315
The specificities of 65 compounds reported to be relatively specific inhibitors of protein kinases have been profiled against a panel of 70-80 protein kinases.... 
Drug discovery | Kinase profiling | Protein kinase | Anti-cancer drugs | Inhibitor specificity | RHO-ASSOCIATED KINASE | TUMOR PROGRESSION | FAMILY-MEMBERS | BIOCHEMISTRY & MOLECULAR BIOLOGY | CELL-PROLIFERATION | protein kinase | P38 MAP KINASE | CYCLIN-DEPENDENT KINASES | RECEPTOR TYROSINE KINASES | drug discovery | kinase profiling | SB 203580 | anti-cancer drugs | ISOFORMS IN-VITRO | P90 RSK | inhibitor specificity | Amino Acid Sequence | Cell Line | Phosphorylation | Recombinant Proteins - antagonists & inhibitors | Animals | Mitogen-Activated Protein Kinases - antagonists & inhibitors | Humans | Drug Design | Protein Kinase Inhibitors - pharmacology | Enzyme Activation | Mitogen-Activated Protein Kinases - metabolism | Spodoptera | Index Medicus | Yes1, Yamaguchi sarcoma viral oncogene homologue 1 | CSK, C-terminal Src kinase | Lck, lymphocyte cell-specific protein-tyrosine kinase | EGF, epidermal growth factor | FGF-R, fibroblast-growth-factor receptor | PAK, p21-activated protein kinase | PDK, 3-phosphoinositide-dependent protein kinase | PI3K, phosphatidylinositol (phosphoinositide) 3-kinase | NEK, NIMA (never in mitosis in Aspergillus nidulans)-related kinase | RSK, p90 ribosomal S6 kinase | HEK-293 cells, human embryonic kidney-293 cells | VEGF, vascular endothelial growth factor (vasoendothelial growth factor) | EF2K, elongation-factor-2 kinase | CK, casein kinase | PTEN, phosphatase and tensin homologue deleted on chromosome 10 | ERK, extracellular-signal-regulated kinase | ATM, ataxia telangiectasia mutated | SRPK, serine-arginine protein kinase | IL-1, interleukin 1 | MNK, MAPK-integrating protein kinase | ROCK, Rho-dependent protein kinase | CaMKK, CaMK kinase | GST, glutathione transferase | MKK1, MAPK kinase-1 (also called MEK1, MAPK or ERK kinase 1) | GAK, cyclin G-associated kinase | FMK, fluoromethylketone | MST, mammalian homologue Ste20-like kinase | PKA, cAMP-dependent protein kinase | FKBP, FK506-binding protein | PPAR, peroxisome-proliferator-activated receptor | IKK, inhibitory κB kinase | PH, pleckstrin homology | MBP, myelin basic protein | AICAR, aminoimidazole-4-carboxamide-1-β-D-ribofuranoside | MAPKAP-K, MAPK-activated protein kinase | Sf21, Spodoptera frugiperda (fall armyworm) 21 | MARK, microtubule-affinity-regulating kinase | PIM, provirus integration site for Moloney murine leukaemia virus | LPS, lipopolysaccharide | MSK, mitogen- and stress-activated protein kinase | MAPK, mitogen-activated protein kinase | MELK, maternal embryonic leucine-zipper kinase | His6, hexahistidine | CAK, cyclin-dependent kinase-activating kinase | Eph-A2, Ephrin A2 receptor | PLK, polo-like kinase | ATF2, activating transcription factor 2 | PKD, protein kinase D | Src, sarcoma kinase | AMPK, AMP-activated protein kinase | MMS, methyl methanesulfonate | CHK, checkpoint kinase | JNK, c-Jun N-terminal kinase | TORC1, mTOR (mammalian target of rapamycin)–raptor (regulatory associated protein of mTOR) complex | BRSK, brain-specific kinase | RIP2, receptor-interacting protein 2 | IGF-1, insulin-like growth factor-1 | S6K1, S6 kinase 1 | DYRK, dual-specificity tyrosine-phosphorylated and -regulated kinase | HIPK, homeodomain-interacting protein kinase | ZMP, aminoimidazole-4-carboxamide-1-β-D-ribofuranoside monophosphate | PRAK, p38-regulated activated kinase | PKC, protein kinase C | Src-I1, Src inhibitor 1 | TANK, TRAF (tumour-necrosis-factor-receptor-associated factor)-family-member-associated nuclear factor κB activator | NFAT, nuclear factor for activated T-cells | PHK, phosphorylase kinase | GSK3, glycogen synthase kinase 3 | PKB, protein kinase B (also called Akt) | CaMK, calmodulin-dependent kinase | CDK, cyclin-dependent protein kinase | NDRG, N-myc downstream-regulated gene | SmMLCK, smooth-muscle myosin light-chain kinase | TBK1, TANK-binding kinase 1 | PRK, protein kinase C-related kinase | SGK, serum- and glucocorticoid-induced kinase
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
Nature, ISSN 0028-0836, 05/2016, Volume 534, Issue 7605, pp. 55 - 62
Somatic mutations have been extensively characterized in breast cancer, but the effects of these genetic alterations on the proteomic landscape remain poorly... 
PATHWAYS | HETEROGENEITY | PIK3CA MUTATIONS | PHOSPHORYLATION | MULTIDISCIPLINARY SCIENCES | GENES | BIOLOGY | RECEPTOR | EXPRESSION | SIGNATURE | REVEALS | Protein Kinases - metabolism | Focal Adhesion Kinase 1 - genetics | Receptor, Epidermal Growth Factor - genetics | Protein Kinases - genetics | Cyclin-Dependent Kinases - metabolism | Receptor, ErbB-2 - genetics | Receptors, G-Protein-Coupled - metabolism | Genomics | Humans | Gene Expression Regulation, Neoplastic | Receptor, ErbB-2 - metabolism | Phosphoproteins - metabolism | Receptor-Interacting Protein Serine-Threonine Kinase 2 - genetics | Tumor Suppressor Protein p53 - genetics | Breast Neoplasms - metabolism | Receptor-Interacting Protein Serine-Threonine Kinase 2 - metabolism | Breast Neoplasms - enzymology | Receptor, Epidermal Growth Factor - metabolism | Phosphoproteins - analysis | Mass Spectrometry | src-Family Kinases - metabolism | Female | Cyclin-Dependent Kinases - genetics | Focal Adhesion Kinase 1 - metabolism | Chromosomes, Human, Pair 5 - genetics | Breast Neoplasms - classification | Chromosome Deletion | p21-Activated Kinases - genetics | Signal Transduction | Molecular Sequence Annotation | Calcium-Binding Proteins - deficiency | Phosphoproteins - genetics | Mutation - genetics | S-Phase Kinase-Associated Proteins - metabolism | p21-Activated Kinases - metabolism | Phosphatidylinositol 3-Kinases - genetics | Breast Neoplasms - genetics | Class I Phosphatidylinositol 3-Kinases | Proteomics | S-Phase Kinase-Associated Proteins - genetics | Receptors, G-Protein-Coupled - genetics | src-Family Kinases - genetics | Calcium-Binding Proteins - genetics | Breast cancer | Genetic aspects | Research | Oncology, Experimental | Cancer | Physiological aspects | Methods | Mutation (Biology) | Proteins | Gene amplification | Peptides | Protein expression | Genomes | Mutation | Kinases | Deoxyribonucleic acid--DNA | Tumors | Index Medicus
Journal Article
Biochemical Journal, ISSN 0264-6021, 01/2005, Volume 385, Issue 2, pp. 399 - 408
We developed a high-throughput HTRF (homogeneous time-resolved fluorescence) assay for Akt kinase activity and screened approx. 270000 compounds for their... 
Allosteric inhibitor | Protein kinase B (PKB) | Inhibitor | Pleckstrin homology domain | Akt | Kinase | PROTEIN-KINASE-B | INDUCED APOPTOSIS | TYROSINE KINASE | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | pleckstrin homology domain | allosteric inhibitor | COWDEN-DISEASE | kinase | inhibitor | STRUCTURAL BASIS | protein kinase B (PKB) | TUMOR-SUPPRESSOR | MOLECULAR-CLONING | CELL-LINE LNCAP | HUMAN CANCER | Phosphoproteins - immunology | Prostatic Neoplasms - chemistry | Humans | Peptides - genetics | Blood Proteins - immunology | Male | Isoenzymes - chemistry | Phosphoproteins - chemistry | Carcinoma - chemistry | Peptides - metabolism | TNF-Related Apoptosis-Inducing Ligand | Blood Proteins - genetics | Adenosine Triphosphate - metabolism | Phosphorylation - drug effects | 3-Phosphoinositide-Dependent Protein Kinases | Protein-Serine-Threonine Kinases - metabolism | Peptides - immunology | Enzyme Inhibitors - pharmacology | Heterocyclic Compounds, 2-Ring - pharmacology | Tumor Necrosis Factor-alpha - pharmacology | Cell Line, Tumor | Prostatic Neoplasms - metabolism | Uterine Cervical Neoplasms - pathology | Quinoxalines - pharmacology | Caspases - metabolism | Uterine Cervical Neoplasms - metabolism | Cloning, Molecular | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Female | Molecular Structure | Carcinoma - pathology | Binding, Competitive | Protein Structure, Tertiary | Proto-Oncogene Proteins - metabolism | Prostatic Neoplasms - pathology | Proto-Oncogene Proteins - antagonists & inhibitors | Peptides - chemistry | Membrane Glycoproteins - pharmacology | Blood Proteins - chemistry | Phosphoproteins - genetics | Enzyme Activation - drug effects | Proto-Oncogene Proteins c-akt | Sequence Homology, Amino Acid | Apoptosis Regulatory Proteins | Signal Transduction - physiology | Uterine Cervical Neoplasms - chemistry | Carcinoma - metabolism | Benzylamines - pharmacology | Isoenzymes - antagonists & inhibitors | Index Medicus | cdk2, cyclin-dependent kinase 2 | FGFR, fibroblast growth factor receptor | MEK, MAPK | SH, Src homology | PI3K, phosphoinositide 3-kinase | DOPS, 1,2-dioleoyl-sn-glycero-3-phospho-L-serine | ERK kinase | DOPC, 1,2-dioleoyl-sn-glycero-3-phosphocholine | DTT, dithiothreitol | PTEN, phosphatase and tensin homologue deleted on chromosome 10 | ERK, extracellular-signal-regulated kinase | PEG, poly(ethylene glycol) | PKC, protein kinase C | FLT, Fms-related tyrosine kinase | lymphoma 1 | GSK3, glycogen synthase kinase 3 | TRAIL, tumour-necrosis-factor-related apoptosis-inducing ligand | HTRF, homogeneous time-resolved fluorescence | PH, pleckstrin homology | MAPKK1, MAPK kinase 1 | FBS, foetal bovine serum | PDK, phosphoinositide-dependent kinase | TCL1, T-cell leukaemia | MAPK, mitogen-activated protein kinase | PKA, protein kinase A | SGK, serum- and glucocorticoid-inducible kinase
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 11/2015, Volume 172, Issue 22, pp. 5265 - 5280
BACKGROUND AND PURPOSE The importance of tyrosine kinases in airway smooth muscle (ASM) contraction is not fully understood. The aim of this study was to... 
RNA INTERFERENCE | GROWTH-FACTOR RECEPTOR | CELLS | ACTIVATION | PROTEIN | PHARMACOLOGY & PHARMACY | ANGIOTENSIN-II | CHANNELS | TYROSINE-PHOSPHORYLATION | MYOSIN PHOSPHATASE | C-SRC | Smooth muscle | Muscle proteins | Phosphotransferases | Myosin | Phosphorylation | Rodents | Research Papers | Research Paper
Journal Article
Molecular and Cellular Biology, ISSN 0270-7306, 02/2002, Volume 22, Issue 4, pp. 992 - 1000
Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley... 
NECROSIS-FACTOR RECEPTOR | ACCESSORY PROTEIN | FAMILY MEMBER | BIOCHEMISTRY & MOLECULAR BIOLOGY | OSTEOPROTEGERIN LIGAND | DEFECTIVE INTERLEUKIN-1 | INTERLEUKIN-1 RECEPTOR | OSTEOCLAST DIFFERENTIATION | ADAPTER PROTEIN | TERMINAL KINASE | C-SRC | CELL BIOLOGY | RNAKL protein | TAB2 protein | TRAF6 protein | TAK1 protein | MAPKK kinase | Cell Growth and Development
Journal Article
FEBS Letters, ISSN 0014-5793, 2001, Volume 496, Issue 1, pp. 44 - 48
The specificity of 4,5,6,7‐tetrabromo‐2‐azabenzimidazole (TBB), an ATP/GTP competitive inhibitor of protein kinase casein kinase‐2 (CK2), has been examined... 
Casein kinase | Inhibitor | Casein kinase-2 | Protein phosphorylation | Protein kinase | nCK, native casein kinase | OA, okadaic acid | PRAK, p38-regulated/activated kinase | CSK, C-terminal Src kinase | AMPK, AMP-activated protein kinase | CHK, checkpoint kinase | JNK, c-Jun N-terminal kinase | MAPKAP, MAPK-activated protein kinase | p70S6K, p70 ribosomal protein S6 kinase | CK, casein kinase | SAPK, stress-activated protein kinase | PDK, 3-phosphoinositide-dependent kinase | DRB, 1-(β | ROCK, Rho-dependent protein kinase | CDK, cyclin-dependent kinase | G-CK, Golgi casein kinase | PKC, protein kinase C | MKK, MAPK kinase (also called MEK) | ribofuranosyl)-5,6-dichlorobenzimidazole | PKA, cAMP-dependent protein kinase | PHK, phosphorylase kinase | GSK3, glycogen synthase kinase 3 | PKB, protein kinase B (also called Akt) | rCK, recombinant casein kinase | ERK, extracellular signal-regulated kinase | HS1, hematopoietic lineage cell-specific protein 1 | MSK, mitogen- and stress-activated protein kinase | TBB, 4,5,6,7-tetrabromo-2-azabenzimidazole or 4,5,6,7-tetrabromobenzotriazole | MAPK, mitogen-activated protein kinase | SGK, serum- and glucocorticoid-induced kinase | CATALYTIC SUBUNIT | ZEA-MAYS | TYROSINE KINASE | CRYSTAL-STRUCTURE | COMPETITIVE INHIBITOR | BIOCHEMISTRY & MOLECULAR BIOLOGY | protein phosphorylation | IMMUNOPHILIN FPR3 | SACCHAROMYCES-CEREVISIAE | protein kinase | CELL BIOLOGY | casein kinase | BIOPHYSICS | inhibitor | CELL-CYCLE | BETA-SUBUNIT | casein kinase-2 | MAMMARY-GLAND | Protein Kinases - metabolism | Jurkat Cells - cytology | Protein Kinases - drug effects | Casein Kinase II | Emodin - pharmacology | Jurkat Cells - metabolism | Humans | Enzyme Inhibitors - pharmacology | Protein-Serine-Threonine Kinases - genetics | Substrate Specificity | Adenosine Triphosphate | Binding Sites - genetics | Binding, Competitive - drug effects | Triazoles - pharmacology | Triazoles - metabolism | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Binding Sites - drug effects | Protein-Serine-Threonine Kinases - metabolism | Staurosporine - pharmacology | Amino Acid Substitution | Jurkat Cells - drug effects | Index Medicus
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2006, Volume 49, Issue 23, pp. 6819 - 6832
Journal Article
FASEB Journal, ISSN 0892-6638, 07/2017, Volume 31, Issue 7, pp. 2963 - 2972
Journal Article
Journal Article
The Journal of Pathology, ISSN 0022-3417, 07/2017, Volume 242, Issue 3, pp. 358 - 370
Focal adhesion kinase ( FAK ) inhibitors have been developed as potential anticancer agents and are undergoing clinical trials. In vitro activation of the FAK... 
tumour angiogenesis | focal adhesion kinase | LOCALIZATION | ACTIVATION | PERMEABILITY | PHOSPHORYLATION | BARRIER FUNCTION | TUMOR ANGIOGENESIS | PATHOLOGY | SRC-FAMILY KINASES | CANCER | ONCOLOGY | SMOOTH-MUSCLE-CELLS | AUTOPHOSPHORYLATION | Cell Division - genetics | Focal Adhesion Kinase 1 - genetics | Neoplasm Transplantation | Antineoplastic Agents, Hormonal - pharmacology | Melanoma - blood supply | Focal Adhesion Protein-Tyrosine Kinases - metabolism | Capillary Permeability - drug effects | Melanoma - enzymology | Endothelium, Vascular - enzymology | Focal Adhesion Protein-Tyrosine Kinases - deficiency | Mutation - genetics | Capillary Permeability - genetics | Focal Adhesion Protein-Tyrosine Kinases - genetics | Homozygote | Neovascularization, Pathologic - enzymology | Animals | Melanoma - genetics | Tamoxifen - pharmacology | Cell Line, Tumor | Neovascularization, Pathologic - genetics | Mice | Cell Hypoxia - genetics | Focal Adhesion Kinase 1 - metabolism | Tyrosine | Fibronectins | Platelet-derived growth factor | Endothelial growth factors | Analysis | Melanoma | Phenols | Genetic aspects | Neovascularization | Permeability | Endothelium | Residues | Phosphorylation | Clinical trials | Activation | Kinases | Blood | Fibronectin | Anticancer properties | Angiogenesis | Antitumor agents | Leakage | Medical research | Vessels | Blood vessels | Tamoxifen | Cadherin | Src protein | Adhesion | Pathology | Signaling | Inhibitors | Hypoxia | In vivo methods and tests | Mutation | Focal adhesion kinase | Paxillin | In vitro methods and tests | Tumors | Index Medicus | Original Paper | Original Papers
Journal Article