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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
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2006, Volume 49, Issue 23, pp. 6819 - 6832
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 07/2017, Volume 23, Issue 14, pp. 3734 - 3743
Purpose: Ibrutinib inhibits Bruton tyrosine kinase (BTK) by irreversibly binding to the Cys-481 residue in the enzyme. However, ibrutinib also inhibits several... 
B-CELLS | ACTIVATION | ONCOLOGY | INITIAL THERAPY | IN-VIVO | X-LINKED AGAMMAGLOBULINEMIA | PCI-32765 | RECEPTOR | OPEN-LABEL | SRC FAMILY KINASES | EXPRESSION | Humans | Pyrazines - administration & dosage | Leukemia, Lymphocytic, Chronic, B-Cell - genetics | Protein Kinase Inhibitors - adverse effects | Benzamides - administration & dosage | Protein-Tyrosine Kinases - genetics | T-Lymphocytes - drug effects | Caspase 3 - genetics | Benzamides - adverse effects | Pyrazoles - adverse effects | Pyrimidines - administration & dosage | src-Family Kinases - antagonists & inhibitors | Leukemia, Lymphocytic, Chronic, B-Cell - pathology | Poly (ADP-Ribose) Polymerase-1 - antagonists & inhibitors | Protein Kinase Inhibitors - administration & dosage | Drug Resistance, Neoplasm - genetics | Pyrazoles - administration & dosage | Signal Transduction - drug effects | Agammaglobulinaemia Tyrosine Kinase | Pyrazines - adverse effects | Pyrimidines - adverse effects | Cell Line, Tumor | Leukemia, Lymphocytic, Chronic, B-Cell - drug therapy | Poly (ADP-Ribose) Polymerase-1 - genetics | Protein-Tyrosine Kinases - antagonists & inhibitors | Drugs | Phosphorylation | Leukocyte migration | Downstream effects | Leukemia | Carbon tetrachloride | Homology | Lymphocytes T | Kinases | Caspase-3 | Biological effects | Lymphocytes | Protein-tyrosine kinase | Downstream | Tyrosine | Chronic lymphatic leukemia | Extracellular signal-regulated kinase | Caspase | Poly(ADP-ribose) polymerase | Cultures | CCL3 protein | Lymphatic leukemia | CCL4 protein | Patients | Bruton's tyrosine kinase | Signaling | Inhibitors | Experimental design | Cell death | Cell migration | Chemokines | Cancer | ibrutinib | apoptosis | Bruton tyrosine kinase | chronic lymphocytic leukemia | acalabrutinib
Journal Article
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 5/2010, Volume 107, Issue 20, pp. 9446 - 9451
Journal Article
Leukemia, ISSN 0887-6924, 03/2009, Volume 23, Issue 3, pp. 477 - 485
The detailed molecular mechanism of action of second-generation BCR-ABL tyrosine kinase inhibitors, including perturbed targets and pathways, should contribute... 
BCR-ABL INHIBITORS | SRC | TYROSINE KINASE | MECHANISMS | NILOTINIB | BREAST-CANCER CELLS | dasatinib | ONCOLOGY | IMATINIB | kinase profiling | RESISTANCE | chronic myeloid leukemia | chemical proteomics | SKI-606 | HEMATOLOGY | bosutinib | Nitriles - pharmacology | Proto-Oncogene Proteins c-abl - antagonists & inhibitors | Humans | Substrate Specificity | Neoplasm Proteins - antagonists & inhibitors | Gene Expression Profiling | K562 Cells - drug effects | Quinolines - pharmacology | Drug Delivery Systems | Leukemia, Myeloid, Accelerated Phase - pathology | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Dasatinib | Nerve Tissue Proteins - antagonists & inhibitors | Aniline Compounds - pharmacology | Leukocytes, Mononuclear - drug effects | Quinolines - chemistry | src-Family Kinases - antagonists & inhibitors | Pyrimidines - pharmacology | Calcium-Calmodulin-Dependent Protein Kinase Type 2 - antagonists & inhibitors | K562 Cells - enzymology | Leukemia, Myeloid, Accelerated Phase - enzymology | Mitogen-Activated Protein Kinases - antagonists & inhibitors | Signal Transduction - drug effects | Fusion Proteins, bcr-abl - antagonists & inhibitors | Nitriles - chemistry | Leukocytes, Mononuclear - enzymology | Protein Kinase Inhibitors - pharmacology | Thiazoles - pharmacology | Aniline Compounds - chemistry | Drug Screening Assays, Antitumor | Protein-Tyrosine Kinases - antagonists & inhibitors | Enzyme inhibitors | Physiological aspects | Chronic myeloid leukemia | Research | Drug therapy | Health aspects | Protein kinases
Journal Article
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 7/2010, Volume 107, Issue 29, pp. 13075 - 13080
Activation of the B-cell antigen receptor (BCR) signaling pathway contributes to the initiation and maintenance of B-cell malignancies and autoimmune diseases.... 
T lymphocytes | Animal models | Disease models | Gels | B lymphocytes | B cell lymphoma | Arthritis | Mice | Autoimmune diseases | Tumors | X-linked agammaglobulinemia | Lymphoma | COLLAGEN-INDUCED ARTHRITIS | THERAPY | RITUXIMAB | MULTIDISCIPLINARY SCIENCES | lymphoma | DOGS | FAMILY KINASES | BTK | RECEPTOR | DEPLETION | MICE | Arthritis, Experimental - drug therapy | Pyrazoles - therapeutic use | Humans | Benzofurans - administration & dosage | Benzofurans - pharmacology | Autoantibodies - biosynthesis | Pyrimidines - chemistry | Benzofurans - chemistry | Protein Kinase Inhibitors - chemistry | Pyrazoles - chemistry | Lymphoma, B-Cell - enzymology | Autoimmune Diseases - drug therapy | Disease Models, Animal | Lymphoma, B-Cell - drug therapy | Pyrazoles - pharmacology | B-Lymphocytes - enzymology | Benzofurans - therapeutic use | Autoimmune Diseases - enzymology | Administration, Oral | Pyrimidines - administration & dosage | Treatment Outcome | Pyrimidines - pharmacology | Receptors, Antigen, B-Cell - immunology | B-Lymphocytes - drug effects | Protein Kinase Inhibitors - administration & dosage | Pyrazoles - administration & dosage | Animals | B-Lymphocytes - immunology | Signal Transduction - drug effects | Lymphocyte Activation - drug effects | Protein Kinase Inhibitors - therapeutic use | Pyrimidines - therapeutic use | Dogs | Protein Kinase Inhibitors - pharmacology | Protein-Tyrosine Kinases - antagonists & inhibitors | Tyrosine | Cell receptors | Models | Lymphomas | Research | Properties | Biological Sciences
Journal Article
Acta Pharmaceutica Sinica B, ISSN 2211-3835, 09/2015, Volume 5, Issue 5, pp. 390 - 401
Since the discovery that non-small cell lung cancer (NSCLC) is driven by epidermal growth factor receptor (EGFR) mutations, the EGFR tyrosine kinase inhibitors... 
Resistance | Mechanisms | TKIs | EGFR | TARGETED THERAPY | ACQUIRED-RESISTANCE | T790M MUTATION | GEFITINIB RESISTANCE | CELL LUNG-CANCER | EPITHELIAL-MESENCHYMAL TRANSITION | GROWTH-FACTOR RECEPTOR | ERLOTINIB RESISTANCE | PHARMACOLOGY & PHARMACY | INTEGRIN BETA1 | TUMOR-GROWTH | ALK, anaplastic lymphoma kinase | BH3, BCL2-homology domain 3 | PDGFRs, platelet-derived growth factor receptors | lymphoma-2 | PDGFs, platelet-derived growth factors | PIK3CA, phosphatidylinositol-4,5-bisphosphate 3-kinase,catalytic subunit alpha | VEGFR, vascular endothelial growth factor receptor | RAF, rapidly accelerated fibrosarcoma | FGFs, fibroblast growth factors | BCL-2, B-cell CLL | IGFBPs, IGF-binding proteins | ERK1 | BIM, BCL2-like 11 | ABCC10, ATP binding cassette, sub-family C, member 10 | ABCC1, ATP binding cassette, sub-family C, member 1 | VEGF, vascular endothelial growth factor | TKs, tyrosine kinases | HER, human epidermal receptor | MEK, mitogen-activated protein kinase | EGFR, epidermal growth factor receptor | BRAF, v-RAF murine sarcoma viral oncogene homolog B1 | AXL, Anexelekto | AKT, protein kinase B | IL, interleukin | TKIs, tyrosine kinase inhibitors | RAS, rat sarcoma | RTK, tyrosine kinase receptor | MAPK, mitogen-activated protein kinase | FGFRs, fibroblast growth factor receptors | SOCS3, suppressor of cytokine signaling 3 | EMT, epithelial mesenchymal transition | IGF, insulin growth factor | Review | 2, extracellular signal-regulated kinases | EML4, echinoderm microtubule-associated protein-like 4 | ABCG2, ATP binding cassette, sub-family G, member 2 | ABCB1, ATP binding cassette, sub-family B, member 1 | BCL2L11 | IL-6R, IL-6 receptor | IGF-1R, IGF-1 receptor | SF, scatter factor | PI3K, phosphatidylinositol-3-kinase | CML, chronic myelogenous leukemia | EGFR-TKIs, epidermal growth factor receptor tyrosine kinase inhibitors | JAK, janus kinase | NSCLC, non-small cell lung cancer | ABC, ATP binding cassette | GAS6, growth-arrest-specific protein 6 | STAT, signal transducers and activators of transcription | EGFRvIII, EGFR variant III | CRKL, Crk-like protein | HGF, hepatocyte growth factor | PTEN, phosphatase and tensin homolog
Journal Article
Journal Article
PLoS ONE, ISSN 1932-6203, 06/2013, Volume 8, Issue 6, p. e66755
Protein kinases play key roles in oncogenic signaling and are a major focus in the development of targeted cancer therapies. Imatinib, a BCR-Abl tyrosine... 
JNK ACTIVATION | IMATINIB-RESISTANT | PROTEIN-TYROSINE KINASES | MEK INHIBITION | MULTIDISCIPLINARY SCIENCES | BCR-ABL | PROTEOMICS ANALYSIS | IKK-ALPHA | NF-KAPPA-B | LYN KINASE | QUANTITATIVE-ANALYSIS | Cell Line | Cell Survival - drug effects | Dasatinib | Protein-Tyrosine Kinases - metabolism | Humans | src-Family Kinases - antagonists & inhibitors | Immunoblotting | NF-kappa B - metabolism | Leukemia - metabolism | Pyrimidines - pharmacology | Reverse Transcriptase Polymerase Chain Reaction | Imatinib Mesylate | Piperazines - pharmacology | Drug Resistance, Neoplasm - genetics | Protein-Tyrosine Kinases - genetics | Chromatography, Affinity | Fusion Proteins, bcr-abl | NF-kappa B - genetics | src-Family Kinases - metabolism | Benzamides - pharmacology | Protein Kinase Inhibitors - pharmacology | Thiazoles - pharmacology | src-Family Kinases - genetics | Antimitotic agents | Tyrosine | Oncology, Experimental | Research | Drug resistance | Drug therapy | Antineoplastic agents | Health aspects | Protein kinases | Cancer | BCR protein | Multiplexing | Adaptations | Protein kinase C | Phosphorylation | Leukemia | Kinases | Interleukin 6 | Proteins | Signal transduction | 2-Methylisoborneol | Inhibition | Fusion protein | Protein-tyrosine kinase | Pharmaceutical sciences | NF-κB protein | Imatinib | Statistical analysis | Myeloid leukemia | Extracellular signal-regulated kinase | Curricula | Mass spectroscopy | Abl protein | JNK protein | Pharmacology | Chronic myeloid leukemia | Gene expression | Medicine | Signaling | Overexpression | Inhibitors | Pharmacy | Proteomics | Scientific imaging | Mutation | Beads | Molecular biology | Mass spectrometry | Viability | Apoptosis
Journal Article
The Journal of pharmacology and experimental therapeutics, ISSN 0022-3565, 11/2017, Volume 363, Issue 2, pp. 240 - 252
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 04/2016, Volume 138, Issue 13, pp. 4608 - 4615
Mutations in the gatekeeper residue of kinases have emerged as a key way through which cancer cells develop resistance to treatment. As such, the design of... 
DESIGN | LIGAND-BINDING | BINDING-AFFINITY PREDICTIONS | MECHANISM | RESISTANCE | FORCE-FIELD | INDUCED FIT | CANCER | CHEMISTRY, MULTIDISCIPLINARY | PROTEIN-KINASES | CONFORMATIONAL SELECTION | Models, Chemical | Computer Simulation | Humans | Drug Design |