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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
International immunopharmacology, ISSN 1567-5769, 2013, Volume 17, Issue 3, pp. 638 - 650
.... Neutrophils express a large number of cell surface receptors for the recognition of pathogen invasion and the inflammatory environment... 
Signaling | Receptors | Inflammation | Kinases | Neutrophils | ACTIVATED PROTEIN-KINASE | COLONY-STIMULATING FACTOR | LEUKOCYTE ADHESION DEFICIENCY | IMMUNOLOGY | SRC-FAMILY KINASES | FORMYL PEPTIDE RECEPTORS | HIGH-AFFINITY RECEPTOR | NOD-LIKE RECEPTORS | BETA-GAMMA-SUBUNIT | TOLL-LIKE RECEPTORS | PHARMACOLOGY & PHARMACY | 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
Biochemical Journal, ISSN 0264-6021, 12/2012, Volume 448, Issue 2, pp. 213 - 220
...) from the insulin receptor family of RTKs (receptor tyrosine kinases), we determined crystal structures of TKDs from TrkA... 
X-ray crystallography | Insulin receptor kinase | Autoinhibition | Receptor tyrosine kinase (RTK) | Receptor tyrosine kinase-like orphan receptor 2 (Ror2) | Tropomyosin receptor kinase A (TrkA) | ALK | ACTIVATION | CRYSTAL-STRUCTURE | TYROSINE KINASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CATALYTIC DOMAIN | autoinhibition | receptor tyrosine kinase-like orphan receptor 2 (Ror2) | CANCER | ANAPLASTIC LYMPHOMA KINASE | insulin receptor kinase | receptor tyrosine kinase (RTK) | MUTATIONS | INHIBITOR | tropomyosin receptor kinase A (TrkA) | EGF RECEPTOR | Neoplasms - metabolism | Humans | Receptor, trkA - antagonists & inhibitors | Crystallography, X-Ray | Antigens, CD - genetics | Antigens, CD - metabolism | Neoplasms - genetics | Receptor, Insulin - genetics | Protein Structure, Quaternary | Antigens, CD - chemistry | Recombinant Proteins - metabolism | Amino Acid Sequence | Catalytic Domain | Recombinant Proteins - antagonists & inhibitors | Receptor Tyrosine Kinase-like Orphan Receptors - metabolism | Models, Molecular | Recombinant Proteins - chemistry | Recombinant Proteins - genetics | Receptor, Insulin - antagonists & inhibitors | Amino Acid Motifs | Receptor Tyrosine Kinase-like Orphan Receptors - antagonists & inhibitors | Receptor Tyrosine Kinase-like Orphan Receptors - chemistry | Receptor, trkA - metabolism | Receptor, Insulin - chemistry | Receptor, trkA - chemistry | Receptor, trkA - genetics | Receptor Tyrosine Kinase-like Orphan Receptors - genetics | Receptor, Insulin - metabolism | Mutation | Enzyme Activation - genetics | In Vitro Techniques | ALK, anaplastic lymphoma kinase | FGFR, fibroblast growth factor receptor | Trk, tropomyosin receptor kinase | C-lobe, C-terminal lobe | EGFR, epidermal growth factor receptor | TKD, tyrosine kinase domain | DTT, dithiothreitol | NSCLC, non-small-cell lung cancer | TCEP, tris-(2-carboxyethyl)phosphine | COSMIC, Catalogue Of Somatic Mutations In Cancer | Ni-NTA, Ni2+-nitrilotriacetate | N-lobe, N-terminal lobe | RTK, receptor tyrosine kinase | CDK, cyclin-dependent kinase | IGF1R, insulin-like growth factor 1 receptor | MuSK, muscle-specific kinase | IRK, insulin receptor kinase | Ror, receptor tyrosine kinase-like orphan receptor
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 science, ISSN 1347-9032, 2016, Volume 107, Issue 8, pp. 1134 - 1140
Journal Article
Cancer Research, ISSN 0008-5472, 10/2004, Volume 64, Issue 19, pp. 7099 - 7109
.... In addition, BAY 43-9006 demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular endothelial growth factor receptor (VEGFR... 
CELLS | ACTIVATION | GENE | ONCOLOGY | SIGNALING PATHWAY | PROTEIN-KINASE | MAP KINASE | B-RAF | INHIBITORS | CANCER | ENDOTHELIAL GROWTH-FACTOR | Niacinamide - analogs & derivatives | Humans | Phenylurea Compounds | Neovascularization, Pathologic - enzymology | Benzenesulfonates - pharmacology | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Receptors, Vascular Endothelial Growth Factor - antagonists & inhibitors | Female | MAP Kinase Kinase Kinases - antagonists & inhibitors | Administration, Oral | Mitogen-Activated Protein Kinase 1 - antagonists & inhibitors | Neoplasms - enzymology | Neoplasms - blood supply | MAP Kinase Kinase Kinases - metabolism | Receptor Protein-Tyrosine Kinases - metabolism | Disease Progression | Proto-Oncogene Proteins c-raf - metabolism | Neoplasms - drug therapy | Xenograft Model Antitumor Assays | Animals | MAP Kinase Signaling System - drug effects | Mitogen-Activated Protein Kinases - antagonists & inhibitors | Mice, Nude | Neovascularization, Pathologic - drug therapy | Cell Line, Tumor | Mice | Proto-Oncogene Proteins c-raf - antagonists & inhibitors | Pyridines - pharmacology | MAP Kinase Kinase Kinase 1 | Mitogen-Activated Protein Kinase 3 | Mitogen-Activated Protein Kinase 1 - metabolism | Mitogen-Activated Protein Kinases - metabolism
Journal Article
Biochemical journal, ISSN 1470-8728, 2009, Volume 420, Issue 3, pp. 345 - 361
RTKs (receptor tyrosine kinases) play important roles in cellular proliferation and differentiation... 
Extracellular-signal-regulated kinase (ERK) | Pleiotrophin | Anaplastic large cell lymphoma (ALCL) | Neuroblastoma | Non-small cell lung cancer (NSLCL) | Midkine | Anaplastic lymphoma kinase (ALK) | Inflammatory myofibroblastic tumour (IMT) | ALK PROTEIN EXPRESSION | inflammatory myofibroblastic tumour (IMT) | NPM-ALK | HEPARIN-BINDING | GROWTH-FACTOR PLEIOTROPHIN | non-small cell lung cancer (NSLCL) | BIOCHEMISTRY & MOLECULAR BIOLOGY | anaplastic lymphoma kinase (ALK) | EML4-ALK FUSION GENE | neuroblastoma | LARGE-CELL LYMPHOMA | extracellular-signal-regulated kinase (ERK) | pleiotrophin | NEUROTROPHIC FACTOR HBNF | INFLAMMATORY MYOFIBROBLASTIC TUMOR | NON-HODGKINS-LYMPHOMA | midkine | anaplastic large cell lymphoma (ALCL) | RECEPTOR TYROSINE KINASE | Carcinoma, Non-Small-Cell Lung - pathology | Lung Neoplasms - genetics | Oncogene Proteins, Fusion - metabolism | Signal Transduction | Carcinoma, Non-Small-Cell Lung - genetics | Protein-Tyrosine Kinases - metabolism | Humans | Lung Neoplasms - metabolism | Neuroblastoma - genetics | Carcinoma, Non-Small-Cell Lung - metabolism | Lung Neoplasms - pathology | Nuclear Proteins - metabolism | Receptor Protein-Tyrosine Kinases | Protein-Tyrosine Kinases - genetics | Models, Biological | Oncogene Proteins, Fusion - genetics | Lymphoma, Large-Cell, Anaplastic - pathology | Neuroblastoma - metabolism | Nuclear Proteins - genetics | Lymphoma, Large-Cell, Anaplastic - metabolism | Neuroblastoma - pathology | Lymphoma, Large-Cell, Anaplastic - genetics | ALK, anaplastic lymphoma kinase | LTK, leucocyte tyrosine kinase | MUC-1, mucin-1 | IRS-1, IR substrate-1 | PTN, pleiotrophin | TGFβ, transforming growth factor β | ERK, extracellular-signal-regulated kinase | PKB, protein kinase B | Shc, Src homology and collagen homology | TPM, tropomyosin | IMP cyclohydrolase | MK, midkine | MYH9, non-muscle myosin heavy chain | MAM, meprin, A5 protein and receptor protein tyrosine phosphatase mu | NPM, nucleophosmin | mTOR, mammalian target of rapamycin | NIPA, nuclear interacting partner of ALK | RPTP, receptor protein tyrosine phosphatase | DLBCL, diffuse large B-cell lymphoma | FOXO3a, forkhead box O 3a | NF-κB, nuclear factor κB | Shp1, SH2 domain-containing phosphatase 1 | RANBP2, Ran-binding protein 2 | ALCL, anaplastic large cell lymphoma | Dpp, decapentaplegic | FRS2, fibroblast growth factor receptor substrate 2 | LDLa, low-density lipoprotein class A | EGFR, epidermal growth factor receptor | SEC31L1, SEC31 homologue A | GIST, gastrointestinal stromal tumour | RTK, receptor tyrosine kinase | SH2, Src homology 2 | TFG, TRK-fused gene | ATIC, 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase | CLTC, clathrin heavy chain | MAPK, mitogen-activated protein kinase | Hen-1, hesitation-1 | MEK, MAPK | PI3K, phosphoinositide 3-kinase | HEK, human embryonic kidney | SCD-2, suppressor of constitutive dauer 2 | Review | EBPβ, CCAAT | CARS, cysteinyl-tRNA synthetase | JNK, c-Jun N-terminal kinase | ERK kinase | Grb2, growthfactor-receptor-bound protein 2 | SCC, squamous cell carcinoma | EML4, echinoderm microtubule-associated protein like 4 | SHH, sonic hedghog | BCR-Abl, breakpoint cluster region-Abl | IR, insulin receptor | ALO17, ALK lymphoma oligomerization partner on chromosome 17 | enhancer-binding protein β | PLCγ, phospholipase Cγ | NSCLC, non-small cell lung cancer | UCN-01, unco-ordinated 1 | Cdc42, cell division cycle 42 | STAT, signal transducer and activator of transcription | DRG, dorsal root ganglia | MSN, moesin | dALK, Drosophila ALK | IL-3, interleukin-3 | CNS, central nervous system | JAK, Janus kinase | CML, chronic myeloid leukaemia | Jeb, jelly belly | IMT, inflammatory myofibroblastic tumour
Journal Article