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gak (23) 23
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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
Biochemical journal, ISSN 1470-8728, 2014, Volume 459, Issue 1, pp. 59 - 69
Cyclin G-associated kinase (GAK) is a regulator of clathrin-coated vesicle trafficking... 
Nanobody | Drug side effect | Kinase inhibitor | Protein structure | Activation loop | Cyclin G-associated kinase | SCANNING FLUOROMETRY | DOMAIN | MECHANISM | cyclin G-associated kinase | BIOCHEMISTRY & MOLECULAR BIOLOGY | VALIDATION | RECEPTOR | nanobody | drug side effect | activation loop | protein structure | REFINEMENT | LIBRARIES | kinase inhibitor | INHIBITORS | PROTEINS | CLATHRIN | Apoproteins - chemistry | Camelus | Protein-Serine-Threonine Kinases - physiology | Humans | Catalytic Domain - physiology | Animals | Apoproteins - physiology | Intracellular Signaling Peptides and Proteins - chemistry | Single-Domain Antibodies - chemistry | Protein Multimerization - physiology | Protein Conformation | Protein-Serine-Threonine Kinases - chemistry | Intracellular Signaling Peptides and Proteins - physiology | Enzyme Activation - physiology | Crystallization - methods | Single-Domain Antibodies - physiology | DARPin, designed ankyrin-repeat protein | AUC, analytical ultracentrifugation | Nb, nanobody | threonine kinase 1 | RU, resonance unit | MPSK1, myristoylated and palmitoylated serine | EGFR, epidermal growth factor receptor | HA, haemagglutinin | SeMet, selenomethionine | TCEP, tris-(2-carboxyethyl)phosphine | NAK, numb-associated kinase | CDR, complementarity-determining region | TEV, Tobacco etch virus | GAK, cyclin G-associated kinase | SPR, surface plasmon resonance | ASCH, activation segment C-terminal helix
Journal Article
ChemistryOpen (Weinheim), ISSN 2191-1363, 2018, Volume 7, Issue 9, pp. 713 - 719
Gefitinib is the molecular target drug for advanced non-smallcell lung cancer. The primary target of gefitinib is the positive mutation of epidermal growth factor receptor, but it also inhibits cyclin G-associated kinase (GAK... 
inhibitor development | protein kinases | complex structures | gefitinib | novel binding sites | GAK | LUNG-CANCER | MUTANT | ACTIVATION | TARGETS | CHEMISTRY, MULTIDISCIPLINARY | INSIGHTS | Epidermal growth factor | Hydrogen | Analysis | Hepatitis C virus | Lung cancer, Non-small cell | Hepatitis C | Gefitinib | Health aspects | Protein kinases | Protein binding | Hepatitis | Hydrogen bonds | Viruses | Activation | Catalytic activity | Disruption | Catalysis | Kinases | Growth factors | Binding sites | Research & development--R&D | Parkinsons disease | Glycerol | Grooves | Proteins | Data collection | Ligands | Software | Mutation
Journal Article
Journal Article
ChemMedChem, ISSN 1860-7179, 2018, Volume 13, Issue 1, pp. 48 - 66
Journal Article
Bioorganic & medicinal chemistry letters, ISSN 0960-894X, 2019, Volume 29, Issue 14, pp. 1727 - 1731
.... We present a focused case study on development of a selective inhibitor of cyclin G associated kinase (GAK) using the quin(az... 
Kinome selectivity | 4-anilinoquinoline | 4-Anilinoquinazoline | Mini-kinome panel | Cyclin G associated kinase (GAK) | MULTIPLE ROLES | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | IDENTIFICATION | Case studies | Drugstores | Quinoline | Medical colleges | Pharmacy
Journal Article
ChemMedChem, ISSN 1860-7187, 2020, Volume 15, Issue 13, pp. 1200 - 1215
.... Herein, we describe the design and testing of a targeted library of 4‐anilinoquin(az)olines for use as inhibitors of cyclin G‐associated kinase (GAK... 
cyclin G-associated kinase (GAK) | anilinoquinazolines | WaterMap | anilinoquinolines | water networks | CHEMISTRY, MEDICINAL | LIGAND-BINDING | PROTEIN | DISCOVERY | SOLVENT | MOLECULES | KLIFS | THERMODYNAMICS | PHARMACOLOGY & PHARMACY | OPTIMIZATION | SELECTIVITY | Design | Inhibitors | Cyclin G | Mapping | Selectivity | Kinases | Drug development | Access routes
Journal Article
Biochemical journal, ISSN 0264-6021, 06/2007, Volume 404, Issue 2, pp. 179 - 190
.... Here we demonstrate that the protein kinase activity of RIP2 has two functions, namely to limit the strength of downstream signalling and to stabilize the active enzyme... 
Pro-inflammatory cytokines | Nucleotide-binding oligomerization domain 2 (NOD2) | Muramyl dipeptide (MDP) | Receptor-interacting protein 2 (RIP2) | Transforming-growth-factor-β-activated kinase-1 (TAK1) | ACTIVATION | CROHNS-DISEASE | muramyl dipeptide (MDP) | BIOCHEMISTRY & MOLECULAR BIOLOGY | NOD2 | P38 MAP KINASE | nucleotide-binding oligomerization domain 2 (NOD2) | TAK1 | pro-inflammatory cytokines | transforming-growth-factor-beta-activated kinase-1 (TAK1) | IN-VIVO | receptor-interacting protein 2 (RIP2) | FRAMESHIFT MUTATION | NF-KAPPA-B | ADAPTIVE IMMUNE-RESPONSES | PROTEIN-KINASE INHIBITORS | Cell Line | Signal Transduction | Humans | Enzyme Inhibitors - pharmacology | Imidazoles - pharmacology | MAP Kinase Kinase Kinases - metabolism | Acetylmuramyl-Alanyl-Isoglutamine - metabolism | DNA Primers | Receptor-Interacting Protein Serine-Threonine Kinase 2 - metabolism | Acetylmuramyl-Alanyl-Isoglutamine - pharmacology | Nod2 Signaling Adaptor Protein - metabolism | Base Sequence | Interleukin-1beta - biosynthesis | Pyridines - pharmacology | Catalysis | Enzyme Activation | Tumor Necrosis Factor-alpha - biosynthesis | Cytokines - biosynthesis | Tumor Necrosis Factor-alpha - antagonists & inhibitors | Interleukin-1beta - antagonists & inhibitors | KI, kinase inactive | CK1, ‘casein kinase 1’ | TLR, Toll-like receptor | WT, wild-type | TNF, tumour necrosis factor | HEK-293, human embryonic kidney 293 cells | JNK, c-Jun N-terminal kinase | MDP, muramyl dipeptide | TAK1, transforming-growth-factor-β-activated kinase-1 | transforming-growth-factor-β-activated kinase-1 (TAK1) | ERK, extracellular-signal-regulated kinase | K63-pUb, Lys63-linked polyubiquitin | RIP2, receptor-interacting protein 2 | MKK1, MAPK kinase-1 | IκB, inhibitor of NF-κB | TAB, TAK1-binding protein | GAK, cyclin G-associated kinase | GAPDH, glyceraldehyde-3-phosphate dehydrogenase | IKKβ, inhibitor of nuclear factor κB kinase β | GST, glutathione S-transferase | NF-κB, nuclear factor κB | NEMO, nuclear factor κB essential modifier | HA, haemagglutinin | NOD, nucleotide-binding oligomerization domain | TRAF6, TNF-receptor-associated factor 6 | M-TriDAP, muramyl-N-acetyl-L-Ala-D-Glu-m-diaminopimelic acid | IL, interleukin | LPS, lipopolysaccharide | shRNA, short hairpin RNA | VSV-G, vesicular-stomatitis-virus envelope glycoprotein | PBMCs, peripheral-blood mononuclear cells | Tpl2, tumour progression locus 2 | FCS, foetal-calf serum | MAPK, mitogen-activated protein kinase
Journal Article
Cellular signalling, ISSN 0898-6568, 04/2014, Volume 26, Issue 4, pp. 716 - 723
Journal Article