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Chemical Science, ISSN 2041-6520, 04/2015, Volume 6, Issue 4, pp. 2449 - 2456
The clinical development of anticancer metallodrugs is often hindered by the elusive nature of their molecular targets. To identify the molecular targets of an... 
ORGANOMETALLIC RUTHENIUM(II) | IN-VITRO | DRUG DISCOVERY | COMPOUND | ANTICANCER METALLODRUGS | REACTIVITY | ICP-MS | BINDING | CHEMISTRY, MULTIDISCIPLINARY | MIDKINE | PROTEIN ADDUCTS | Proteins | Antiproliferatives | Proteomics | Histones | Fibroblasts | Guanines | Ruthenium organometallic complexes | Cancer
Journal Article
Nature Chemical Biology, ISSN 1552-4450, 01/2017, Volume 13, Issue 2, pp. 133 - 134
  The ability to measure the binding of a compound to its intended target in live cells or tissue is a critical parameter for drug discovery. A new method... 
DRUG | CELL | BIOCHEMISTRY & MOLECULAR BIOLOGY | Microscopy | Drug Delivery Systems | Fluorescence | Pharmaceutical sciences
Journal Article
Nature Chemical Biology, ISSN 1552-4450, 02/2017, Volume 13, Issue 2, pp. 133 - 134
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 03/2018, Volume 61, Issue 6, pp. 2533 - 2551
Recent literature has both suggested and questioned MTH1 as a novel cancer target. BAY-707 was just published as a target validation small molecule probe for... 
OXIDATIVE STRESS | CHEMISTRY, MEDICINAL | LIGAND-BINDING | PERMEABILITY | METABOLISM | CANCER-CELL SURVIVAL | HOT-SPOTS | ANTICANCER STRATEGY | DISCOVERY | ARYLAMINES | PREDICTION
Journal Article
Nature methods, ISSN 1548-7091, 11/2015, Volume 12, Issue 11, pp. 1055 - 1057
Thermal stabilization of proteins upon ligand binding provides an efficient means to assess binding of small molecules to proteins. We show here that in... 
target deconvolution | metabolite | proteomics | drug discovery | network
Journal Article
Nature Chemical Biology, ISSN 1552-4450, 07/2015, Volume 11, Issue 8, pp. 536 - 541
Journal Article
Journal Article
Nature, ISSN 0028-0836, 2014, Volume 508, Issue 7495, pp. 222 - 227
Activated RAS GTPase signalling is a critical driver of oncogenic transformation and malignant disease. Cellular models of RAS-dependent cancers have been used... 
CELL LUNG-CANCER | RAS-TRANSFORMATION | OVEREXPRESSION | OXIDATIVE STRESS | HMTH1 | MESSENGER-RNA | GENE | MULTIDISCIPLINARY SCIENCES | HUMAN MUTT HOMOLOG | TUMORIGENESIS | SMALL-MOLECULE INHIBITION | ras Proteins - genetics | Colonic Neoplasms - genetics | Proto-Oncogene Proteins p21(ras) | Pyridines - chemistry | Colonic Neoplasms - drug therapy | Humans | Substrate Specificity | DNA Breaks, Single-Stranded - drug effects | Protein Kinase Inhibitors - chemistry | Pyrazoles - chemistry | Phosphoric Monoester Hydrolases - biosynthesis | DNA Repair Enzymes - metabolism | Female | Antineoplastic Agents - pharmacology | DNA Repair Enzymes - antagonists & inhibitors | Homeostasis - drug effects | Aminoquinolines - pharmacology | DNA Repair Enzymes - chemistry | Disease Models, Animal | Phosphoric Monoester Hydrolases - antagonists & inhibitors | Pyrazoles - pharmacology | Crystallization | Models, Molecular | Proto-Oncogene Proteins - genetics | Antineoplastic Agents - chemistry | Mice, SCID | Nucleotides - metabolism | Xenograft Model Antitumor Assays | Animals | Colonic Neoplasms - pathology | DNA Repair | DNA Repair Enzymes - biosynthesis | Proteomics | Protein Conformation | Mice | Protein Kinase Inhibitors - pharmacology | Pyridines - pharmacology | Phosphoric Monoester Hydrolases - metabolism | Phosphoric Monoester Hydrolases - chemistry | Crizotinib | Enzymes | Colon cancer | Physiological aspects | Genetic aspects | Research | Nucleotides | Studies | Oxidative stress | Inhibitor drugs | Medical prognosis | Homeostasis | Mutation | Kinases | Experiments | Cancer | Life Sciences | crizotinib | cancer | stereoselectivity | MTH1 | DNA repair | drug
Journal Article
Methods in Molecular Biology, ISSN 1064-3745, 01/2016, Volume 1394, pp. 211 - 218
Chemical proteomics provides a powerful means to gain systems-level insight into the mode of action of small molecules and/or natural products. In contrast to... 
Target deconvolution | Drug discovery | Chemical proteomics | Mode of action | Proteome | Animals | Proteins - chemistry | Proteomics - methods | Humans
Journal Article
Nature Chemical Biology, ISSN 1552-4450, 08/2015, Volume 11, Issue 8, pp. 571 - 578
textabstractThe CEBPA gene is mutated in 9% of patients with acute myeloid leukemia (AML). Selective expression of a short (30-kDa) CCAAT-enhancer binding... 
DNA-BINDING | PROTEIN | HISTONE H3 | BIOCHEMISTRY & MOLECULAR BIOLOGY | IN-VIVO | MYELOID DIFFERENTIATION | SELF-RENEWAL | MIXED-LINEAGE LEUKEMIA | PROTEOMIC IDENTIFICATION | EXPRESSION | H3K4 METHYLTRANSFERASE ACTIVITY | Small Molecule Libraries - pharmacology | Myeloid-Lymphoid Leukemia Protein - metabolism | Humans | Leukemia, Myeloid, Acute - metabolism | Gene Expression Regulation, Neoplastic | Molecular Sequence Data | Molecular Targeted Therapy | Histone-Lysine N-Methyltransferase - antagonists & inhibitors | Protein Isoforms - metabolism | Biphenyl Compounds - pharmacology | Antineoplastic Agents - pharmacology | CCAAT-Enhancer-Binding Proteins - genetics | Tumor Cells, Cultured | CCAAT-Enhancer-Binding Proteins - metabolism | Protein Structure, Tertiary | Amino Acid Sequence | Histone-Lysine N-Methyltransferase - genetics | Signal Transduction | Leukemia, Myeloid, Acute - pathology | Animals | Histones - genetics | Histone-Lysine N-Methyltransferase - metabolism | Cell Differentiation - drug effects | Myeloid-Lymphoid Leukemia Protein - genetics | Dihydropyridines - pharmacology | Protein Binding | Cell Proliferation - drug effects | Mice | Molecular Docking Simulation | Histones - metabolism | Mutation | Leukemia, Myeloid, Acute - genetics | Myeloid-Lymphoid Leukemia Protein - antagonists & inhibitors | Protein Isoforms - genetics | Index Medicus
Journal Article