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Angewandte Chemie (International ed.), ISSN 1433-7851, 2015, Volume 54, Issue 24, pp. 7114 - 7119
...‐guided synthesis by in situ click chemistry is combined with synthetic epitope targeting to exploit the tertiary structure of the BoNT protein as a landscape for assembling a competitive inhibitor. A substrate... 
epitope targeting | peptides | botulinum neurotoxin | combinatorial screening | target‐guided synthesis | Target-guided synthesis | Botulinum neurotoxin | Epitope targeting | Combinatorial screening | Peptides | target-guided synthesis | EXOCYTOSIS | NEUROTRANSMITTER RELEASE | STRATEGY | TETANUS | IDENTIFICATION | CHEMISTRY, MULTIDISCIPLINARY | CAPTURE AGENTS | SITU | SEROTYPE | Epitopes - metabolism | Humans | Neurons - cytology | Botulinum Toxins, Type A - antagonists & inhibitors | Enzyme Inhibitors - chemical synthesis | Botulinum Toxins, Type A - drug effects | Peptides - chemical synthesis | Enzyme Inhibitors - chemistry | Cell Differentiation | Neurons - metabolism | Induced Pluripotent Stem Cells - cytology | Neurons - drug effects | Induced Pluripotent Stem Cells - metabolism | Protein Structure, Tertiary | Amino Acid Sequence | Catalytic Domain | Induced Pluripotent Stem Cells - drug effects | Peptides - chemistry | Click Chemistry | Cells, Cultured | Enzyme Inhibitors - pharmacology | Peptides - pharmacology | Protein Binding | Ligands | Epitopes - chemistry | Botulinum Toxins, Type A - metabolism | Microscopy, Fluorescence | Antigenic determinants | Botulism | Index Medicus | Proteins | Inhibitors | Synthesis | Toxins | Intoxication | Inhibition | Screens
Journal Article
Xenobiotica, ISSN 1366-5928, 2008, Volume 38, Issue 7-8, pp. 802 - 832
.... Recent insights into the structural features of P-gp/MDR1 enable a re-evaluation of the biochemical evidence on the binding and transport of drugs by P-gp/MDR1. 2... 
blood-brain barrier | pharmacokinetics | P-glycoprotein (P-gp) | intestinal absorption | single nucleotide polymorphism | Single nucleotide polymorphism | Blood-brain barrier | Intestinal absorption | Pharmacokinetics | ORGANIC ANION TRANSPORTER | C3435T POLYMORPHISM | CYSTEINE-SCANNING MUTAGENESIS | TRANSMEMBRANE DOMAIN | BLOOD-BRAIN-BARRIER | TENOFOVIR DISOPROXIL FUMARATE | MDR1 GENE | PHARMACOLOGY & PHARMACY | TOXICOLOGY | ABC TRANSPORTERS | MULTIDRUG-RESISTANCE GENE | TERTIARY STRUCTURE CHANGES | Neoplasms - metabolism | Organ Specificity - drug effects | Drug Resistance, Multiple - drug effects | Humans | Biological Availability | Structure-Activity Relationship | Neoplasm Proteins - metabolism | Xenobiotics - pharmacokinetics | Neoplasms - chemistry | Organ Specificity - genetics | Neoplasms - genetics | Gene Expression Regulation, Neoplastic - drug effects | Neoplasm Proteins - genetics | ATP Binding Cassette Transporter, Subfamily B, Member 1 - chemistry | Gene Expression Regulation, Neoplastic - genetics | Drug Resistance, Multiple - genetics | Neoplasm Proteins - chemistry | Protein Structure, Tertiary - genetics | Substrate Specificity - genetics | ATP Binding Cassette Transporter, Subfamily B | ATP Binding Cassette Transporter, Subfamily B, Member 1 - genetics | ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism | Drug Resistance, Neoplasm - genetics | Substrate Specificity - drug effects | Polymorphism, Single Nucleotide | Drug Resistance, Neoplasm - drug effects
Journal Article
Bioorganic & medicinal chemistry letters, ISSN 0960-894X, 2014, Volume 24, Issue 16, pp. 3891 - 3897
Journal Article
Nature (London), ISSN 1476-4687, 2016, Volume 535, Issue 7610, pp. 153 - 158
Inflammatory caspases (caspases 1, 4, 5 and 11) are activated in response to microbial infection and danger signals. When activated, they cleave mouse and... 
LISTERIA-MONOCYTOGENES | INTERLEUKIN-1-BETA | MULTIDISCIPLINARY SCIENCES | MIXED LINEAGE KINASE | PERFORIN | NLRP3 INFLAMMASOME | INTRACELLULAR BACTERIA | GRANZYMES | CASPASE-1 ACTIVATION | GRANULYSIN | CELL-DEATH | Conserved Sequence - genetics | Inflammasomes - metabolism | Phosphatidylinositol Phosphates - metabolism | Pyroptosis - drug effects | Escherichia coli - drug effects | Humans | Molecular Sequence Data | Neoplasm Proteins - pharmacology | Escherichia coli - cytology | Neoplasm Proteins - metabolism | Escherichia coli - metabolism | Protein Multimerization - genetics | Listeria monocytogenes - metabolism | Cell Membrane - metabolism | Membrane Proteins - metabolism | Listeria monocytogenes - cytology | Porosity - drug effects | Neoplasm Proteins - genetics | Cell Membrane - drug effects | Staphylococcus aureus - metabolism | Amino Acid Sequence | Cell Line | Microbial Viability - drug effects | Membrane Proteins - genetics | Mice, Inbred C57BL | Phosphatidylserines - metabolism | Neoplasm Proteins - chemistry | Cardiolipins - metabolism | Cell Membrane - ultrastructure | Protein Structure, Tertiary - genetics | Microscopy, Electron | Pyroptosis - genetics | Protein Transport | Liposomes - chemistry | Animals | Membrane Proteins - chemistry | Cell Membrane Permeability - drug effects | Staphylococcus aureus - cytology | Liposomes - metabolism | Mice | Mutation | Staphylococcus aureus - drug effects | Listeria monocytogenes - drug effects | Observations | Apoptosis | Proteins | Membranes | Bacterial infections | Immunology | Plasmids | Bacteria | Infections | Cells
Journal Article
Nature (London), ISSN 0028-0836, 08/2014, Volume 512, Issue 7514, pp. 333 - 337
Journal Article
Nature (London), ISSN 1476-4687, 2016, Volume 535, Issue 7613, pp. 517 - 522
Journal Article
Nature (London), ISSN 1476-4687, 2013, Volume 497, Issue 7448, pp. 217 - 223
.... Here we report co-crystal structures of a complex of truncated mTOR and mammalian lethal with SEC13 protein 8 (mLST8... 
MAMMALIAN TARGET | RAPAMYCIN | RAPTOR | BINDING PARTNER | RAG GTPASES | RHEB | PATHWAY | TOR | MULTIDISCIPLINARY SCIENCES | CELL-GROWTH | P70 S6 KINASE | Adaptor Proteins, Signal Transducing - chemistry | Catalytic Domain - drug effects | TOR Serine-Threonine Kinases - metabolism | Pyridines - chemistry | Furans - pharmacology | Humans | Crystallography, X-Ray | Structure-Activity Relationship | Pyrimidines - chemistry | TOR Serine-Threonine Kinases - antagonists & inhibitors | Indoles - metabolism | Furans - chemistry | Adenosine Triphosphate - metabolism | Indoles - pharmacology | Tacrolimus Binding Protein 1A - pharmacology | Naphthyridines - chemistry | Ribosomal Protein S6 Kinases, 70-kDa - metabolism | Purines - metabolism | Purines - pharmacology | MTOR Associated Protein, LST8 Homolog | Tacrolimus Binding Protein 1A - chemistry | Models, Molecular | Magnesium - metabolism | Pyrimidines - pharmacology | Sirolimus - metabolism | Sirolimus - pharmacology | Magnesium - chemistry | Purines - chemistry | TOR Serine-Threonine Kinases - chemistry | Tacrolimus Binding Protein 1A - metabolism | Pyridines - pharmacology | Sirolimus - chemistry | Adaptor Proteins, Signal Transducing - metabolism | Adenosine Triphosphate - chemistry | Indoles - chemistry | Naphthyridines - pharmacology | Naphthyridines - metabolism | Protein Structure, Tertiary - drug effects | Proteins | Enzymes | Kinases | Crystal structure
Journal Article