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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 | 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
Biochemical Journal, ISSN 0264-6021, 01/2007, Volume 401, Issue 1, pp. 29 - 38
Hormones and growth factors induce the activation of a number of protein kinases that belong to the AGC subfamily, including isoforms of PKA, protein kinase B... 
Kinase-specific inhibitor | Phosphorylation | p90 ribosomal S6 kinase (RSK) | BI-D1870 | Mitogen-activated protein kinase (MAPK) | ACTIVATED PROTEIN-KINASE | MAP KINASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | mitogen-activated protein kinase (MAPK) | MSK1 | INDUCTION | IDENTIFICATION | INACTIVATION | CREB | GROWTH | BI-DI870 | SUPPRESSES | phosphorylation | kinase-specific inhibitor | Cell Line | Pteridines - pharmacology | Humans | Enzyme Inhibitors - pharmacology | Morpholines - pharmacology | Rats | Ribosomal Protein S6 Kinases, 90-kDa - metabolism | Animals | Ribosomal Protein S6 Kinases, 90-kDa - genetics | Ribosomal Protein S6 Kinases, 90-kDa - antagonists & inhibitors | Protein Kinase Inhibitors - pharmacology | Enzyme Activation | Kinetics | Chromones - pharmacology | Isoenzymes - antagonists & inhibitors | MES, mouse embryonic stem | PI3K, phosphoinositide 3-kinase | EGF, epidermal growth factor | PKA, cAMP-dependent protein kinase A | FKHR, forkhead in rhabdosarcoma transcription factor | RSK, p90 ribosomal S6 kinase | JNK, c-Jun N-terminal kinase | CREB, cAMP-response-element-binding protein | SGK1, serum- and glucocorticoid-induced kinase-1 | PDK1, phosphoinositide-dependent kinase 1 | PKB, protein kinase B | Lck, lymphocyte kinase | ROCK, Rho-dependent protein kinase | MKK1, MAPK kinase-1 | protein kinase G | AGC, cAMP-dependent protein kinase | protein kinase C | HEK-293, human embryonic kidney 293 | ERK1, extracellular-signal-regulated kinase 1 | GST, glutathione S-transferase | PKC, protein kinase C | S6K, p70 ribosomal S6 kinase | PH, pleckstrin homology | PLK1, polo-like kinase 1 | CK1, casein kinase-1 | FBS, foetal bovine serum | MSK, mitogen- and stress-activated protein kinase | CDK2–A, cyclin-dependent kinase 2 complexed with cyclin A | DYRK1a, dual-specificity tyrosine-phosphorylated and -regulated kinase 1a | GSK3α, glycogen synthase kinase 3α | MAPK, mitogen-activated protein kinase
Journal Article
Journal of Neuroscience, ISSN 0270-6474, 03/2004, Volume 24, Issue 13, pp. 3370 - 3378
The mechanisms of action of human synthetic and naturally secreted cell-derived amyloid beta-peptide (Abeta)(1-42) on the induction of long-term potentiation... 
Metabotropic glutamate receptors | Cdk5 | JNK | LTP | Amyloid β-protein | Alzheimer's disease | p38 MAPK | Hippocampus | NEURONAL APOPTOSIS | hippocampus | ALZHEIMERS-DISEASE | MAP KINASE | metabotropic glutamate receptors | amyloid beta-protein | SYNAPTIC PLASTICITY | FREQUENCY STIMULATION | AREA CA1 | NEUROSCIENCES | IN-VITRO | PATHWAY | MICE | PRECURSOR PROTEIN | Receptors, Metabotropic Glutamate - drug effects | Cyclin-Dependent Kinases - metabolism | Amyloid beta-Peptides - pharmacology | Humans | Amyloid beta-Peptides - secretion | Peptide Fragments - pharmacology | Receptors, Metabotropic Glutamate - metabolism | Hippocampus - drug effects | Ovary - cytology | Excitatory Postsynaptic Potentials - drug effects | Cyclin-Dependent Kinases - drug effects | Dose-Response Relationship, Drug | Excitatory Postsynaptic Potentials - physiology | Long-Term Potentiation - drug effects | Amyloid beta-Peptides - genetics | JNK Mitogen-Activated Protein Kinases | Long-Term Potentiation - physiology | Receptor, Metabotropic Glutamate 5 | Female | Electric Stimulation - methods | Peptide Fragments - genetics | p38 Mitogen-Activated Protein Kinases | CHO Cells | Ovary - metabolism | Cricetinae | Enzyme Inhibitors - pharmacology | Peptide Fragments - secretion | Rats | Excitatory Amino Acid Antagonists - pharmacology | Cyclin-Dependent Kinase 5 | Animals | Ovary - secretion | Hippocampus - physiology | In Vitro Techniques | Mitogen-Activated Protein Kinases - drug effects | Mitogen-Activated Protein Kinases - metabolism | Plasticity | Development | amyloid β-protein | Repair
Journal Article
Nature, ISSN 0028-0836, 03/2010, Volume 464, Issue 7287, pp. 431 - 435
Activating mutations in KRAS and BRAF are found in more than 30% of all human tumours and 40% of melanoma, respectively, thus targeting this pathway could have... 
SELECTIVE INHIBITOR | POTENT | EFFICACY | MECHANISM | PHOSPHORYLATION | MULTIDISCIPLINARY SCIENCES | KINASE | C-RAF | B-RAF | MUTATIONS | PROTEINS | Neoplasms - metabolism | ras Proteins - genetics | Proto-Oncogene Proteins p21(ras) | Diphenylamine - pharmacology | raf Kinases - antagonists & inhibitors | Humans | Protein Multimerization | ras Proteins - metabolism | Protein Transport - drug effects | Extracellular Signal-Regulated MAP Kinases - metabolism | raf Kinases - metabolism | Diphenylamine - analogs & derivatives | Mitogen-Activated Protein Kinase Kinases - metabolism | Adenosine Triphosphate - metabolism | Indoles - pharmacology | Benzamides - pharmacology | Cell Membrane - metabolism | raf Kinases - genetics | Cell Membrane - drug effects | Proto-Oncogene Proteins B-raf - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Pyrazoles - pharmacology | Protein Structure, Tertiary | Proto-Oncogene Proteins - metabolism | Cell Line | Indenes - pharmacology | raf Kinases - chemistry | Proto-Oncogene Proteins c-raf - genetics | Mitogen-Activated Protein Kinase Kinases - antagonists & inhibitors | Neoplasms - enzymology | Proto-Oncogene Proteins - genetics | Enzyme Activation - drug effects | Sulfonamides - pharmacology | Proto-Oncogene Proteins c-raf - metabolism | Neoplasms - drug therapy | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Xenograft Model Antitumor Assays | Animals | MAP Kinase Signaling System - drug effects | Protein Kinase Inhibitors - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Proto-Oncogene Proteins c-raf - deficiency | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Neoplasms - pathology | Ras genes | Growth | Physiological aspects | Cellular signal transduction | Genetic aspects | Research | Mitogen-activated protein kinases | Competition | Clinical trials | Enzymes | Kinases | Proteins | Cellular | Inhibitors | Pathways | Tumours | Signalling | Dimerization
Journal Article
International Immunopharmacology, ISSN 1567-5769, 11/2013, Volume 17, Issue 3, pp. 638 - 650
Neutrophils play a critical role in the host defense against bacterial and fungal infections, but their inappropriate activation also contributes to tissue... 
Signaling | Receptors | Inflammation | Kinases | Neutrophils | ACTIVATED PROTEIN-KINASE | COLONY-STIMULATING FACTOR | LEUKOCYTE ADHESION DEFICIENCY | IMMUNOLOGY | SRC-FAMILY KINASES | HUMAN POLYMORPHONUCLEAR LEUKOCYTES | HIGH-AFFINITY RECEPTOR | TUMOR-NECROSIS-FACTOR | TOLL-LIKE RECEPTORS | PHARMACOLOGY & PHARMACY | BETA-GAMMA-SUBUNITS | NF-KAPPA-B | Signal Transduction - immunology | Animals | Receptors, Cell Surface - immunology | Humans | Neutrophils - immunology | Selectins - immunology | Mycoses | Lectins | Fc receptors | Integrins | FcR, Fc-receptor | GPI, glycosylphosphatidylinositol anchor | CLEC, C-type lectin | OSCAR, osteoclast-associated receptor | PKB, protein kinase B | DAG, diacyl-glycerol | Tyk2, tyrosine protein kinase 2 | VCAM-1, vascular cell adhesion molecule 1 | ICAM-1, intercellular adhesion molecule 1 | FADD, Fas-associated protein with death domain | IκB, inhibitor of NF-κB | GM-CSF, granulocyte | MyD88, myeloid differentiation protein 88 | TNF, tumor necrosis factor | LTβ, lymphotoxin β | TRADD, TNFR1-associated death domain protein | Abl, Abelson leukemia proto-oncogene | SLP-76, SH2 domain-containing leukocyte protein of 76 kDa | CALDAG-GEFI, calcium and DAG-regulated guanine nucleotide exchange factor I | IL, interleukin | Src, Rous sarcoma virus proto-oncogene | IRF, IFN regulatory factor | RIG, retinoic acid-inducible gene | PLC, phospholipase C | TCR, T-cell receptor | IKK, IκB kinase | ITAM, immunoreceptor tyrosine-based activation motif | CARD, caspase activation and recruitment domain | IP3, inositol-tris-phosphate | CHO, Chinese hamster ovary cells | MKK, MAP kinase kinase | fMLP, formly-Met-Leu-Phe | TRAF, TNF receptor-associated factor | MIP, macrophage inflammatory protein | Rac, Ras-related C3 botulinum toxin substrate | monocyte colony-stimulating factor | PIP3, phosphatidylinositol-3-phosphate | VLA-4, very late antigen 4 (α4β1 integrin) | PAF, platelet activating factor | STAT, signal transducer and activator of transcription | TAK, TGFβ-activated kinase 1 | Mac-1, macrophage antigen 1 (αMβ2 integrin) | FcRγ, Fc-receptor γ-chain | Asc, apoptosis-associated speck-like protein containing a CARD | cIAP, cellular inhibitor of apoptosis | BCR, B-cell receptor | Fgr, Gardner–Rasheed feline sarcoma proto-oncogene | VASP, vasodilator-stimulated phosphoprotein | Hck, hematopoietic cell kinase | TGFβ, transforming growth factor β | Rap, Ras-related protein | SHP-1, SH2 domain-containing protein tyrosine phosphatase 1 | Syk, spleen tyrosine kinase | GPCR, G protein-coupled receptor | G-CSF, granulocyte colony-stimulating factor | TREM, triggering receptor expressed on myeloid cells | DISC, death-inducing signaling complex | MDL-1, myeloid DAP12-associating lectin 1 | C3G, Crk SH3 domain-binding guanine nucleotide exchange factor (RapGEF1) | NF-κB, nuclear factor κB | ERM, ezrin-radixin-moesin | Epac1, exchange protein activated by cyclic AMP 1 | LTB4, leukotriene B4 | Mcl, macrophage C-type lectin | SAP130, Sin3A-associated protein of 130 kDa | SH2, Src-homology 2 domain | MAP kinase, mitogen-activated protein kinase | PSGL-1, P-selectin glycoprotein ligand | PI3K, phoshoinositide-3-kinase | ADAP, adhesion and degranulation promoting adapter protein (Fyb, SLAP-130) | NLRP3, NOD-like receptor family, pyrin domain containing 3 | MDA5, melanoma differentiation-associated protein 5 | TLR, Toll-like receptor | GRK, GPCR kinase | LAD, leukocyte adhesion deficiency | MAPKAP-kinase, MAP kinase-associated protein kinase | ZAP-70, ζ-chain-associated protein of 70 kDa | TRAIL, TNF-related apoptosis-inducing ligand | JNK, c-Jun N-terminal kinase | LFA-1, lymphocyte function-associated receptor 1 (αLβ2 integrin) | ROS, reactive oxygen species | RIP3, receptor-interacting serine-threonine protein kinase 3 | DAP12, DNAX activating protein 12 | IFN, interferon | PIR, paired immunoglobulin-like receptor | PKC, protein kinase C | PAK, p21-activated kinase | ESL-1, E-selectin ligand 1 | GAP, GTPase activating protein | ERK, extracellular signal-regulated kinase | SOCS, suppressor of cytokine signaling | JAK, Janus kinase | RANK, receptor activator of NF-κB | IRAK, IL-1 receptor-associated kinase | NOD, nucleotide-binding oligomerization domain containing protein | CEACAM3, carcinoembryonic antigen-related cell adhesion molecule 3 (CD66b)
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 | 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