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Biochemical journal, ISSN 1470-8728, 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 | 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
Nature reviews. Cancer, ISSN 1474-1768, 2017, Volume 17, Issue 2, pp. 93 - 115
.... Proliferation depends on progression through four distinct phases of the cell cycle G0/G1, S, G2 and M which is regulated by several cyclin-dependent kinases (CDKs... 
INVESTIGATIONAL AURORA KINASE | PHASE-II TRIAL | POLO-LIKE-KINASE | EARLY EMBRYONIC-DEVELOPMENT | DINACICLIB SCH 727965 | ADVANCED SOLID TUMORS | ONCOLOGY | PREVENTS TUMOR-GROWTH | VOLASERTIB BI 6727 | DEPENDENT KINASE INHIBITOR | SMALL-MOLECULE INHIBITOR | Cyclin-Dependent Kinase 6 - antagonists & inhibitors | Humans | Checkpoint Kinase 1 - physiology | Aurora Kinase A - antagonists & inhibitors | Cyclin-Dependent Kinase 2 - physiology | Cell Cycle Proteins - antagonists & inhibitors | Protein-Tyrosine Kinases - physiology | Aurora Kinase A - physiology | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Cyclin-Dependent Kinase 4 - antagonists & inhibitors | Proto-Oncogene Proteins - antagonists & inhibitors | Signal Transduction | Protein-Serine-Threonine Kinases - physiology | Checkpoint Kinase 1 - antagonists & inhibitors | Clinical Trials as Topic | Neoplasms - drug therapy | Animals | Cyclin-Dependent Kinase 4 - physiology | Nuclear Proteins - antagonists & inhibitors | Proto-Oncogene Proteins - physiology | Cyclin-Dependent Kinase 2 - antagonists & inhibitors | Cyclin-Dependent Kinase 6 - physiology | Nuclear Proteins - physiology | Cell Cycle Proteins - physiology | Protein-Tyrosine Kinases - antagonists & inhibitors | Proteins | Care and treatment | Usage | MicroRNA | Cell cycle | Research | Cancer
Journal Article
Journal Article
The Journal of clinical investigation, ISSN 0021-9738, 2015, Volume 125, Issue 5, pp. 1780 - 1789
Kinase inhibitors have played an increasingly prominent role in the treatment of cancer and other diseases... 
MEDICINE, RESEARCH & EXPERIMENTAL | ONCOGENIC ACTIVATION | PROTEIN-KINASE | TUMOR-INFILTRATING MACROPHAGES | ADAPTIVE RESISTANCE | ACQUIRED-RESISTANCE | CLINICAL RESISTANCE | DIACYLGLYCEROL KINASES | RECEPTOR TYROSINE KINASE | IMATINIB MESYLATE | ANTITUMOR EFFICACY | Immunotherapy - methods | Apoptosis - drug effects | Humans | Substrate Specificity | Drug Resistance, Neoplasm | Neoplasm Proteins - antagonists & inhibitors | Antineoplastic Agents - therapeutic use | Antineoplastic Combined Chemotherapy Protocols - pharmacology | Neoplasms - genetics | Protein Processing, Post-Translational - drug effects | Drug Design | Antineoplastic Agents - pharmacology | Gene Expression Regulation, Neoplastic - drug effects | Phosphorylation - drug effects | Neoplasm Proteins - genetics | Molecular Targeted Therapy - methods | Neoplasms - enzymology | Gene Fusion | Enzyme Activation - drug effects | Neoplasms - drug therapy | Drug Synergism | Point Mutation | Gene Amplification | Signal Transduction - drug effects | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Oncogene Proteins, Fusion - genetics | Protein Kinase Inhibitors - therapeutic use | Oncogene Proteins, Fusion - antagonists & inhibitors | Signal Transduction - physiology | Protein Kinase Inhibitors - pharmacology | Apoptosis - physiology | Enzyme inhibitors | Physiological aspects | Research | Drug therapy | Phosphotransferases | Health aspects | Cancer | Proteins | Phosphorylation | Gene amplification | Biology | Regulation | Genomes | Mutation | Metastasis | Kinases | Phosphatase | Tumors | Review
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... 
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 | ROCK, Rho-dependent protein kinase | CDK, cyclin-dependent kinase | G-CK, Golgi casein kinase | PKC, protein kinase C | MKK, MAPK kinase (also called MEK) | PKA, cAMP-dependent protein kinase | DRB, 1-(β-D-ribofuranosyl)-5,6-dichlorobenzimidazole | 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
Journal Article
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 metastatic solid tumors, including patients... 
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
Cancer cell, ISSN 1535-6108, 2010, Volume 17, Issue 6, pp. 547 - 559
In mice, Lkb1 deletion and activation of Kras G12D results in lung tumors with a high penetrance of lymph node and distant metastases. We analyzed these... 
CELLCYCLE | SIGNALING | INACTIVATION | SUPPRESSOR | SIGNATURES | ONCOLOGY | SRC | ADENOCARCINOMA | SENSITIVITY | MUTATIONS | LKB1/STK11 | EXPRESSION | TUMORIGENESIS | CELL BIOLOGY | 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
Journal Article