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Cancer cell, ISSN 1535-6108, 2011, Volume 19, Issue 1, pp. 17 - 30
...) and 2-hydroxyglutarate (2-HG), respectively. Here we demonstrate that 2-HG is a competitive inhibitor of multiple α... 
BREAST-CANCER | TRANSCRIPTIONAL ACTIVITY | IDH2 MUTATIONS | ONCOLOGY | PROLYL HYDROXYLATION | INTEGRATED GENOMIC ANALYSIS | 2-OXOGLUTARATE OXYGENASES | ACUTE MYELOID-LEUKEMIA | HIF-ALPHA | HISTONE DEMETHYLATION | FAMILY | CELL BIOLOGY | Dioxygenases - metabolism | Histone Demethylases - antagonists & inhibitors | Gene Expression - genetics | Caenorhabditis elegans Proteins - chemistry | Humans | Ketoglutaric Acids - chemistry | Glioma - genetics | F-Box Proteins | Oxidoreductases, N-Demethylating - antagonists & inhibitors | Ketoglutaric Acids - pharmacology | Cytosine - metabolism | Hypoxia-Inducible Factor 1, alpha Subunit - metabolism | Glutarates - chemistry | Oxidoreductases, N-Demethylating - metabolism | DNA-Binding Proteins - antagonists & inhibitors | Glioma - enzymology | Endostatins - metabolism | Models, Molecular | Isocitrate Dehydrogenase - genetics | Histone Demethylases - metabolism | Dioxygenases - antagonists & inhibitors | Amino Acid Substitution - physiology | Procollagen-Proline Dioxygenase - genetics | Cell Line, Tumor | Isocitrate Dehydrogenase - metabolism | Glutarates - pharmacology | Histones - metabolism | Jumonji Domain-Containing Histone Demethylases - metabolism | Caenorhabditis elegans - enzymology | Cytosine - analogs & derivatives | Gene Expression - drug effects | Caenorhabditis elegans Proteins - metabolism | Isocitrate Dehydrogenase - antagonists & inhibitors | Glioma - metabolism | Procollagen-Proline Dioxygenase - metabolism | DNA-Binding Proteins - metabolism | Mixed Function Oxygenases | Biocatalysis - drug effects | Jumonji Domain-Containing Histone Demethylases - antagonists & inhibitors | Jumonji Domain-Containing Histone Demethylases - chemistry | Procollagen-Proline Dioxygenase - antagonists & inhibitors | Ketoglutaric Acids - metabolism | Oxalates - pharmacology | Binding, Competitive | Proto-Oncogene Proteins - metabolism | Proto-Oncogene Proteins - antagonists & inhibitors | Catalytic Domain | Proto-Oncogene Proteins - genetics | Hypoxia-Inducible Factor-Proline Dioxygenases | DNA-Binding Proteins - genetics | Homeodomain Proteins - genetics | Animals | 5-Methylcytosine - metabolism | Caenorhabditis elegans Proteins - antagonists & inhibitors | Glutarates - metabolism
Journal Article
Journal Article
Cancer Research, ISSN 0008-5472, 04/2013, Volume 73, Issue 8, pp. 2574 - 2586
.... Here, we report the characterization of Torin2, a second-generation ATP-competitive inhibitor that is potent and selective for mTOR with a superior pharmacokinetic profile to previous inhibitors... 
MAMMALIAN TARGET | CANCER-CELLS | RAPAMYCIN MTOR | SIGNALING PATHWAYS | THERAPY | PI3K | ONCOLOGY | HIGHLY POTENT | MUTATIONS | ANTITUMOR-ACTIVITY | DISCOVERY | Lung Neoplasms - drug therapy | ras Proteins - genetics | Tumor Suppressor Proteins - antagonists & inhibitors | Apoptosis - drug effects | Humans | Lung Neoplasms - metabolism | Lung Neoplasms - pathology | Antineoplastic Agents - administration & dosage | Autophagy - drug effects | Cell Cycle Proteins - antagonists & inhibitors | TOR Serine-Threonine Kinases - antagonists & inhibitors | Protein Kinase Inhibitors - chemistry | Adenosine Triphosphate - metabolism | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Tumor Burden - genetics | Antineoplastic Agents - pharmacology | Proto-Oncogene Proteins c-akt - metabolism | Disease Models, Animal | Binding, Competitive | Lung Neoplasms - genetics | Naphthyridines - chemistry | DNA-Binding Proteins - antagonists & inhibitors | Ataxia Telangiectasia Mutated Proteins | Drug Synergism | Xenograft Model Antitumor Assays | Protein Kinase Inhibitors - administration & dosage | Animals | Tumor Burden - drug effects | Cell Line, Tumor | Protein Binding | Benzimidazoles - pharmacology | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Kinetics | Cell Cycle - drug effects | Naphthyridines - administration & dosage | Naphthyridines - pharmacology | Proto-Oncogene Proteins c-akt - antagonists & inhibitors | lung cancer | mTOR | ATM | kinase inhibitors | ATR
Journal Article
Proceedings of the National Academy of Sciences - PNAS, ISSN 0027-8424, 2019, Volume 116, Issue 30, pp. 201901744 - 15022
Phosphorylation reactions, driven by competing kinases and phosphatases, are central elements of cellular signal transduction. We reconstituted a native... 
bistability | ACTIVATION | MEMBRANE | MULTIDISCIPLINARY SCIENCES | OCRL | HIGH-AFFINITY BINDING | kinase | PHOSPHATIDYLINOSITOL 4-PHOSPHATE | SIGNALING SYSTEM | LIGATION-INDEPENDENT CLONING | NUCLEOTIDE EXCHANGE FACTOR | stochastic | polarization | phosphatase | DIFFUSION | FEEDBACK | Phosphorylation | Phosphatidylinositol Phosphates - metabolism | Phosphotransferases (Alcohol Group Acceptor) - chemistry | Humans | Bacterial Proteins - chemistry | Unilamellar Liposomes - chemistry | Single Molecule Imaging | Phosphatidylinositol Phosphates - chemistry | Phosphatidylinositol 4,5-Diphosphate - metabolism | Stochastic Processes | Guanine Nucleotide Exchange Factors - metabolism | Legionella pneumophila - enzymology | Phosphatidylinositol 4,5-Diphosphate - chemistry | Legionella pneumophila - chemistry | Recombinant Proteins - metabolism | Signal Transduction | Recombinant Proteins - chemistry | Phosphotransferases (Alcohol Group Acceptor) - metabolism | Unilamellar Liposomes - metabolism | Phospholipase C delta - metabolism | Phospholipase C delta - chemistry | Bacterial Proteins - metabolism | Kinetics | Lipid Bilayers - chemistry | Lipid Bilayers - metabolism | Phosphoric Monoester Hydrolases - metabolism | Guanine Nucleotide Exchange Factors - chemistry | Phosphoric Monoester Hydrolases - chemistry | Phosphates | Cellular signal transduction | Phosphatases | Phosphotransferases | Polarization | Membranes | Confinement | Composition | Copy number | Variations | Lipids | Membrane composition | Kinases | Phosphatase | Signalling systems | Bistability | Signal transduction | Lipid kinase | Transduction | Stochasticity | Diffusion | Biological Sciences | PNAS Plus
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Journal Article
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