Nature Chemistry, ISSN 1755-4330, 2014, Volume 6, Issue 6, pp. 460 - 461
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NATURE CHEMISTRY, ISSN 1755-4330, 06/2014, Volume 6, Issue 6, pp. 460 - 461
Journal Article
ISSN 2041-6520, 10/2019, Volume 1, Issue 41, pp. 9591 - 9596
A large proportion of medicinally relevant molecules bear nitrogen and sp 3 -hybridized carbon functionalities. Overwhelmingly, these atoms are found as part...
Journal Article
Chemical Science, ISSN 2041-6520, 01/2019, Volume 10, Issue 41, pp. 9591 - 9596
A large proportion of medicinally relevant molecules bear nitrogen and sp3-hybridized carbon functionalities. Overwhelmingly, these atoms are found as part of...
Hydrogen bonds | Imines | Lithium | Iridium | Aldehydes | Nitrogen | Carbon | Substrates | Alkylation
Hydrogen bonds | Imines | Lithium | Iridium | Aldehydes | Nitrogen | Carbon | Substrates | Alkylation
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Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect
Nature, ISSN 0028-0836, 05/2010, Volume 465, Issue 7294, pp. 96 - 100
The worldwide prevalence of chronic hepatitis C virus (HCV) infection is estimated to be approaching 200 million people(1). Current therapy relies upon a...
DOMAIN | REPLICATION | HEPATITIS-C VIRUS | RNA | MULTIDISCIPLINARY SCIENCES | CELL | NONSTRUCTURAL PROTEINS | Hepatitis C - drug therapy | Humans | Middle Aged | Drug Resistance, Viral | Imidazoles - chemistry | Cercopithecus aethiops | Male | Young Adult | Time Factors | Antiviral Agents - chemistry | Inhibitory Concentration 50 | Adult | Female | Vero Cells | Hepacivirus - drug effects | Cell Line | Antiviral Agents - pharmacology | Antiviral Agents - blood | Antiviral Agents - therapeutic use | Genotype | Imidazoles - pharmacology | Imidazoles - blood | Animals | Adolescent | Hepatitis C - virology | HeLa Cells | Viral Load - drug effects | Viral Nonstructural Proteins - antagonists & inhibitors | Biochemical genetics | Genetic aspects | Research | Hepatitis C virus | RNA polymerases | Genotype & phenotype | Amino acids
DOMAIN | REPLICATION | HEPATITIS-C VIRUS | RNA | MULTIDISCIPLINARY SCIENCES | CELL | NONSTRUCTURAL PROTEINS | Hepatitis C - drug therapy | Humans | Middle Aged | Drug Resistance, Viral | Imidazoles - chemistry | Cercopithecus aethiops | Male | Young Adult | Time Factors | Antiviral Agents - chemistry | Inhibitory Concentration 50 | Adult | Female | Vero Cells | Hepacivirus - drug effects | Cell Line | Antiviral Agents - pharmacology | Antiviral Agents - blood | Antiviral Agents - therapeutic use | Genotype | Imidazoles - pharmacology | Imidazoles - blood | Animals | Adolescent | Hepatitis C - virology | HeLa Cells | Viral Load - drug effects | Viral Nonstructural Proteins - antagonists & inhibitors | Biochemical genetics | Genetic aspects | Research | Hepatitis C virus | RNA polymerases | Genotype & phenotype | Amino acids
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 12/2013, Volume 54, Issue 49, p. 6722
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NATURE CHEMICAL BIOLOGY, ISSN 1552-4450, 10/2019, Volume 15, Issue 10, pp. 937 - 944
Targeted protein degradation as a therapeutic modality has seen dramatic progress and massive investment in recent years because of the convergence of two key...
COMPLEX | SELECTIVE DEGRADATION | STRUCTURAL BASIS | BIOCHEMISTRY & MOLECULAR BIOLOGY | GLUTAMINE-SYNTHETASE | LENALIDOMIDE | OKIHIRO-SYNDROME | THALIDOMIDE | CEREBLON | PROTAC DESIGN | E3 UBIQUITIN LIGASE | Proteins | Degradation | Ubiquitin | Binding | Proteolysis | Chimeras | Binders | Ubiquitin-protein ligase | Optimization | Substrates
COMPLEX | SELECTIVE DEGRADATION | STRUCTURAL BASIS | BIOCHEMISTRY & MOLECULAR BIOLOGY | GLUTAMINE-SYNTHETASE | LENALIDOMIDE | OKIHIRO-SYNDROME | THALIDOMIDE | CEREBLON | PROTAC DESIGN | E3 UBIQUITIN LIGASE | Proteins | Degradation | Ubiquitin | Binding | Proteolysis | Chimeras | Binders | Ubiquitin-protein ligase | Optimization | Substrates
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Nature Chemical Biology, ISSN 1552-4450, 07/2015, Volume 11, Issue 7, pp. 511 - 517
Spinal muscular atrophy (SMA), which results from the loss of expression of the survival of motor neuron-1 (SMN1) gene, represents the most common genetic...
SURVIVAL | SYSTEM | PROTEIN | SPINAL MUSCULAR-ATROPHY | MESSENGER-RNA | GENE | BIOCHEMISTRY & MOLECULAR BIOLOGY | IDENTIFICATION | EXPRESSION | BINDING | SINGLE NUCLEOTIDE | RNA Precursors - chemistry | Ribonucleoprotein, U1 Small Nuclear - metabolism | Small Molecule Libraries - pharmacology | Alternative Splicing | Humans | Small Molecule Libraries - metabolism | Survival of Motor Neuron 2 Protein - metabolism | Proteolysis | Survival of Motor Neuron 2 Protein - chemistry | Protein Binding - drug effects | Survival of Motor Neuron 2 Protein - genetics | Ribonucleoprotein, U1 Small Nuclear - chemistry | Female | RNA Precursors - metabolism | RNA, Double-Stranded - metabolism | Binding Sites | RNA, Double-Stranded - chemistry | Disease Models, Animal | RNA, Double-Stranded - agonists | Muscular Atrophy, Spinal - mortality | Gene Expression | Muscular Atrophy, Spinal - metabolism | Ribonucleoprotein, U1 Small Nuclear - agonists | Models, Molecular | Small Molecule Libraries - chemical synthesis | Mice, Transgenic | RNA Precursors - agonists | Muscular Atrophy, Spinal - pathology | Animals | Protein Stability - drug effects | Survival Analysis | Muscular Atrophy, Spinal - drug therapy | Mice | Molecular biology | Rodents | Neurological disorders
SURVIVAL | SYSTEM | PROTEIN | SPINAL MUSCULAR-ATROPHY | MESSENGER-RNA | GENE | BIOCHEMISTRY & MOLECULAR BIOLOGY | IDENTIFICATION | EXPRESSION | BINDING | SINGLE NUCLEOTIDE | RNA Precursors - chemistry | Ribonucleoprotein, U1 Small Nuclear - metabolism | Small Molecule Libraries - pharmacology | Alternative Splicing | Humans | Small Molecule Libraries - metabolism | Survival of Motor Neuron 2 Protein - metabolism | Proteolysis | Survival of Motor Neuron 2 Protein - chemistry | Protein Binding - drug effects | Survival of Motor Neuron 2 Protein - genetics | Ribonucleoprotein, U1 Small Nuclear - chemistry | Female | RNA Precursors - metabolism | RNA, Double-Stranded - metabolism | Binding Sites | RNA, Double-Stranded - chemistry | Disease Models, Animal | RNA, Double-Stranded - agonists | Muscular Atrophy, Spinal - mortality | Gene Expression | Muscular Atrophy, Spinal - metabolism | Ribonucleoprotein, U1 Small Nuclear - agonists | Models, Molecular | Small Molecule Libraries - chemical synthesis | Mice, Transgenic | RNA Precursors - agonists | Muscular Atrophy, Spinal - pathology | Animals | Protein Stability - drug effects | Survival Analysis | Muscular Atrophy, Spinal - drug therapy | Mice | Molecular biology | Rodents | Neurological disorders
Journal Article
Angewandte Chemie International Edition, ISSN 1433-7851, 11/2016, Volume 55, Issue 46, pp. 14218 - 14238
Can classical and modern chemical C−H oxidation reactions complement biotransformation in the synthesis of drug metabolites? We have surveyed the literature in...
C−H functionalization | biotransformation | chemotransformation | drug discovery | drug metabolites | HYDROXYLATED ARENES | LEAD DIVERSIFICATION | UDENFRIEND SYSTEM | FUNGAL PEROXYGENASES | C-H functionalization | TERT-BUTYL HYDROPEROXIDE | CHEMISTRY, MULTIDISCIPLINARY | BENZYLIC OXIDATION | CYTOCHROME-P450 ENZYMES | ORGANIC-COMPOUNDS | LATE-STAGE FUNCTIONALIZATION | ACTIVE METABOLITE | Microfluidic Analytical Techniques | Transition Elements - chemistry | Biological Products - chemistry | Pharmaceutical Preparations - metabolism | Electrochemical Techniques | Oxidation-Reduction | Pharmaceutical Preparations - chemistry | Biological Products - metabolism | Catalysis | Hydrogen - chemistry | Carbon - chemistry | Electrochemical reactions | Metabolites | Liver | Electrochemistry | Oxidation-reduction reaction | Drug discovery | Pharmaceutical industry | Microfluidics | Oxidation
C−H functionalization | biotransformation | chemotransformation | drug discovery | drug metabolites | HYDROXYLATED ARENES | LEAD DIVERSIFICATION | UDENFRIEND SYSTEM | FUNGAL PEROXYGENASES | C-H functionalization | TERT-BUTYL HYDROPEROXIDE | CHEMISTRY, MULTIDISCIPLINARY | BENZYLIC OXIDATION | CYTOCHROME-P450 ENZYMES | ORGANIC-COMPOUNDS | LATE-STAGE FUNCTIONALIZATION | ACTIVE METABOLITE | Microfluidic Analytical Techniques | Transition Elements - chemistry | Biological Products - chemistry | Pharmaceutical Preparations - metabolism | Electrochemical Techniques | Oxidation-Reduction | Pharmaceutical Preparations - chemistry | Biological Products - metabolism | Catalysis | Hydrogen - chemistry | Carbon - chemistry | Electrochemical reactions | Metabolites | Liver | Electrochemistry | Oxidation-reduction reaction | Drug discovery | Pharmaceutical industry | Microfluidics | Oxidation
Journal Article
Nature Communications, ISSN 2041-1723, 2015, Volume 6, Issue 1, p. 5943
Alkaloids constitute a large family of natural products possessing diverse biological properties. Their unique and complex structures have inspired numerous...
ORGANIC-SYNTHESIS | ACTIVATION | ASYMMETRIC-SYNTHESIS | DIVERSIFICATION | NATURAL-PRODUCTS | MULTIDISCIPLINARY SCIENCES | BOND FUNCTIONALIZATION | CHEMISTRY | ALPHA-AMINO-ACID | HETEROARENES SCOPE | DISCOVERY | Amines - chemistry | Biological Products - chemistry | Chemistry, Pharmaceutical - methods | Magnetic Resonance Spectroscopy | Strychnine - chemistry | Drug Design | Catalysis | Hydrogen - chemistry | Alkaloids - chemistry | Carbon - chemistry | Rhodium - chemistry | Strychnine - analogs & derivatives
ORGANIC-SYNTHESIS | ACTIVATION | ASYMMETRIC-SYNTHESIS | DIVERSIFICATION | NATURAL-PRODUCTS | MULTIDISCIPLINARY SCIENCES | BOND FUNCTIONALIZATION | CHEMISTRY | ALPHA-AMINO-ACID | HETEROARENES SCOPE | DISCOVERY | Amines - chemistry | Biological Products - chemistry | Chemistry, Pharmaceutical - methods | Magnetic Resonance Spectroscopy | Strychnine - chemistry | Drug Design | Catalysis | Hydrogen - chemistry | Alkaloids - chemistry | Carbon - chemistry | Rhodium - chemistry | Strychnine - analogs & derivatives
Journal Article
Nature Cell Biology, ISSN 1465-7392, 10/2014, Volume 16, Issue 11, pp. 1069 - 1079
Cells rely on autophagy to clear misfolded proteins and damaged organelles to maintain cellular homeostasis. In this study we use the new autophagy inhibitor...
SYSTEM | LYSOSOMES | PHOSPHATIDYLINOSITOL 3-PHOSPHATE | CROHN-DISEASE | UBIQUITIN | KINASE | RECEPTOR | IDENTIFICATION | GENOME-WIDE ASSOCIATION | DELETION | CELL BIOLOGY | Nuclear Receptor Coactivators - metabolism | Humans | Phagosomes - metabolism | Cells, Cultured | Autophagy - physiology | Iron - metabolism | Autophagy - drug effects | Animals | Ferritins - metabolism | Lysosomes - metabolism | Homeostasis - physiology | Protein Binding | Class III Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Mice | Homeostasis | Autophagy (Cytology) | Genetic aspects | Properties | Ferritin
SYSTEM | LYSOSOMES | PHOSPHATIDYLINOSITOL 3-PHOSPHATE | CROHN-DISEASE | UBIQUITIN | KINASE | RECEPTOR | IDENTIFICATION | GENOME-WIDE ASSOCIATION | DELETION | CELL BIOLOGY | Nuclear Receptor Coactivators - metabolism | Humans | Phagosomes - metabolism | Cells, Cultured | Autophagy - physiology | Iron - metabolism | Autophagy - drug effects | Animals | Ferritins - metabolism | Lysosomes - metabolism | Homeostasis - physiology | Protein Binding | Class III Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Mice | Homeostasis | Autophagy (Cytology) | Genetic aspects | Properties | Ferritin
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 08/2013, Volume 56, Issue 15, pp. 6007 - 6021
The medicinal chemistry subgroup of the American Chemical Society’s Green Chemistry Institute Pharmaceutical Roundtable (ACS GCI PR) offers a perspective on...
REPLACEMENT | ORGANIC-SYNTHESIS | ROOM-TEMPERATURE | CHEMISTRY, MEDICINAL | CROSS-COUPLINGS | PERSPECTIVE | ENZYMATIC REDUCTION | GREEN CHEMISTRY | DRUG DISCOVERY | PHARMACEUTICAL-INDUSTRY | SOLVENT | Chemistry, Pharmaceutical - methods | Green Chemistry Technology - methods | Chemical Engineering - trends | Green Chemistry Technology - trends | Drug Discovery - trends | Drug Discovery - methods | Chemical Engineering - methods | Chemistry, Pharmaceutical - trends
REPLACEMENT | ORGANIC-SYNTHESIS | ROOM-TEMPERATURE | CHEMISTRY, MEDICINAL | CROSS-COUPLINGS | PERSPECTIVE | ENZYMATIC REDUCTION | GREEN CHEMISTRY | DRUG DISCOVERY | PHARMACEUTICAL-INDUSTRY | SOLVENT | Chemistry, Pharmaceutical - methods | Green Chemistry Technology - methods | Chemical Engineering - trends | Green Chemistry Technology - trends | Drug Discovery - trends | Drug Discovery - methods | Chemical Engineering - methods | Chemistry, Pharmaceutical - trends
Journal Article
Angewandte Chemie, ISSN 0044-8249, 11/2016, Volume 128, Issue 46, p. 14430
Können klassische und moderne C-H-Oxidationsreaktionen Biotransformationen bei der Synthese von Wirkstoffmetaboliten ergänzen? Wir haben versucht, bei einer...
Journal Article
CHEMICAL SCIENCE, ISSN 2041-6520, 11/2019, Volume 10, Issue 41, pp. 9591 - 9596
A large proportion of medicinally relevant molecules bear nitrogen and sp(3)-hybridized carbon functionalities. Overwhelmingly, these atoms are found as part...
MEDICINAL CHEMISTS TOOLBOX | NATURAL-PRODUCT | SUBSTITUTION | THIOMORPHOLINES | VOLTAMMETRIC OXIDATION | HANTZSCH 1,4-DIHYDROPYRIDINES | COUPLED ELECTRON-TRANSFER | SINGLE-LAYER | SNAP REAGENTS | EFFICIENT | CHEMISTRY, MULTIDISCIPLINARY
MEDICINAL CHEMISTS TOOLBOX | NATURAL-PRODUCT | SUBSTITUTION | THIOMORPHOLINES | VOLTAMMETRIC OXIDATION | HANTZSCH 1,4-DIHYDROPYRIDINES | COUPLED ELECTRON-TRANSFER | SINGLE-LAYER | SNAP REAGENTS | EFFICIENT | CHEMISTRY, MULTIDISCIPLINARY
Journal Article
Nature Chemical Biology, ISSN 1552-4450, 10/2018, Volume 14, Issue 10, pp. 981 - 987
Targeted protein degradation via small-molecule modulation of cereblon offers vast potential for the development of new therapeutics. Cereblon-binding...
MULTIPLE-MYELOMA | CONGENITAL-ABNORMALITIES | GENE | RADIAL RAY SYNDROME | PROTEIN-DEGRADATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | LENALIDOMIDE | OKIHIRO-SYNDROME | MUTATIONS | RENAL-OCULAR SYNDROME | E3 UBIQUITIN LIGASE | Binding | Epidemics | Rabbits | Congenital defects | Transgenic mice | Birth defects | Birth | Phocomelia | Drug development | Substrates | Zinc | Teratogenicity | Mice | Zinc finger proteins | Mutation | Thalidomide | Index Medicus
MULTIPLE-MYELOMA | CONGENITAL-ABNORMALITIES | GENE | RADIAL RAY SYNDROME | PROTEIN-DEGRADATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | LENALIDOMIDE | OKIHIRO-SYNDROME | MUTATIONS | RENAL-OCULAR SYNDROME | E3 UBIQUITIN LIGASE | Binding | Epidemics | Rabbits | Congenital defects | Transgenic mice | Birth defects | Birth | Phocomelia | Drug development | Substrates | Zinc | Teratogenicity | Mice | Zinc finger proteins | Mutation | Thalidomide | Index Medicus
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