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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
Nature Reviews Cancer, ISSN 1474-175X, 01/2017, Volume 17, Issue 2, pp. 93 - 115
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
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 | 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
Nature Communications, ISSN 2041-1723, 05/2016, Volume 7, Issue 1, p. 11363
No effective targeted therapies exist for cancers with somatic KRAS mutations. Here we develop a synthetic lethal chemical screen in isogenic KRAS-mutant and... 
CELL LUNG-CANCER | SURVIVAL | COMBINATION THERAPY | STRATEGY | MULTIDISCIPLINARY SCIENCES | SYNTHETIC LETHAL INTERACTION | RESISTANCE | MUTATIONS | RAS ONCOGENES | EXPRESSION | REVEALS | Lung Neoplasms - drug therapy | Proto-Oncogene Proteins p21(ras) - genetics | Humans | Male | Antineoplastic Agents - administration & dosage | Lung Neoplasms - physiopathology | G2 Phase - drug effects | Tumor Suppressor Protein p53 - genetics | rho-Associated Kinases - antagonists & inhibitors | Cell Cycle Proteins - antagonists & inhibitors | Enzyme Inhibitors - administration & dosage | Cyclin-Dependent Kinase Inhibitor p21 - genetics | rho-Associated Kinases - metabolism | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Cell Cycle Proteins - genetics | Cyclin-Dependent Kinase Inhibitor p21 - metabolism | Female | Protein-Serine-Threonine Kinases - metabolism | Proto-Oncogene Proteins p21(ras) - metabolism | Lung Neoplasms - genetics | Proto-Oncogene Proteins - metabolism | Proto-Oncogene Proteins - antagonists & inhibitors | Lung Neoplasms - enzymology | Mice, Inbred C57BL | Cell Cycle Proteins - metabolism | Protein-Serine-Threonine Kinases - genetics | Tumor Suppressor Protein p53 - metabolism | rho-Associated Kinases - genetics | Proto-Oncogene Proteins - genetics | Cell Division - drug effects | Animals | Proto-Oncogene Proteins p21(ras) - antagonists & inhibitors | Mice | Mice, Inbred BALB C | Mutation | Transcription | Polo-like kinase 1 | Lung cancer | Cyclin-dependent kinases | RhoA protein | Kinases | Rho-associated kinase | Cyclin-dependent kinase | Organic chemistry | Synergistic effects | Cyclin-dependent kinase inhibitor p21 | Transfection | DNA microarrays | Polo-like kinase | Rocks | Inhibition | Tumors | Cancer
Journal Article
Journal Article
Cell Death and Differentiation, ISSN 1350-9047, 03/2012, Volume 19, Issue 3, pp. 369 - 377
Journal Article
Cell Cycle, ISSN 1538-4101, 12/2010, Volume 9, Issue 23, pp. 4720 - 4734
Journal Article