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Nature Communications, ISSN 2041-1723, 04/2016, Volume 7, Issue 1, p. 11360
The prenyl-binding protein PDEδ is crucial for the plasma membrane localization of prenylated Ras. Recently, we have reported that the small-molecule... 
Small Molecule Libraries - pharmacology | Epithelial Cells - metabolism | Proto-Oncogene Proteins p21(ras) - genetics | Pyrazoles - chemical synthesis | Antineoplastic Agents - chemical synthesis | Epithelial Cells - drug effects | Humans | Pancreatic Ducts - drug effects | Gene Expression Regulation, Neoplastic | Cyclic Nucleotide Phosphodiesterases, Type 6 - antagonists & inhibitors | Crystallography, X-Ray | Cyclic Nucleotide Phosphodiesterases, Type 6 - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 6 - genetics | Pancreatic Ducts - pathology | Benzimidazoles - chemistry | Pancreatic Ducts - metabolism | Pyrazoles - chemistry | Proto-Oncogene Proteins p21(ras) - chemistry | Phosphodiesterase Inhibitors - chemical synthesis | Antineoplastic Agents - pharmacology | Protein Interaction Domains and Motifs | Phosphodiesterase Inhibitors - chemistry | Binding Sites | Proto-Oncogene Proteins p21(ras) - metabolism | Pyrazoles - pharmacology | Recombinant Proteins - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 6 - metabolism | Gene Expression | Protein Structure, Secondary | Signal Transduction | Phosphodiesterase Inhibitors - pharmacology | Recombinant Proteins - chemistry | Small Molecule Libraries - chemical synthesis | Epithelial Cells - pathology | Recombinant Proteins - genetics | Antineoplastic Agents - chemistry | Pyrazines - chemical synthesis | Pyrazines - chemistry | Small Molecule Libraries - chemistry | Proto-Oncogene Proteins p21(ras) - antagonists & inhibitors | Cell Line, Tumor | Protein Binding | Benzimidazoles - pharmacology | Molecular Docking Simulation | Pyrazines - pharmacology
Journal Article
Journal of Pharmaceutical and Biomedical Analysis, ISSN 0731-7085, 01/2014, Volume 87, pp. 176 - 190
Journal Article
Mini-Reviews in Medicinal Chemistry, ISSN 1389-5575, 06/2015, Volume 15, Issue 9, pp. 762 - 775
The chemistry of 1,3,4-thiadiazoles is very well known. A universal and commonly used method of the synthesis of different 2,5-disubstituted 1,3,4-thiadiazoles... 
1,3,4-thiadiazoles | Cyclooxygenase inhibitors | Leishmanicidal agents | Metalloproteinases inhibitors | Anticonvulsant activity | Diuretics | Carbonic anhydrase inhibitors | Anticancer agents | VITRO ANTITUBERCULOSIS ACTIVITY | CHEMISTRY, MEDICINAL | leishmanicidal agents | GYNECOLOGIC-ONCOLOGY-GROUP | SELECTIVE PDE7 INHIBITORS | HELICOBACTER-PYLORI ACTIVITY | HUMAN ISOFORM-II | IN-VITRO | metalloproteinases inhibitors | anticonvulsant activity | carbonic anhydrase inhibitors | diuretics | AMINOPEPTIDASE-N INHIBITORS | cyclooxygenase inhibitors | SUBSTITUTED 1,3,4-THIADIAZOLES | CARBONIC-ANHYDRASE INHIBITORS | Phosphodiesterase Inhibitors - therapeutic use | Carbonic Anhydrase Inhibitors - chemistry | Humans | Matrix Metalloproteinase Inhibitors - chemistry | Antineoplastic Agents - therapeutic use | Cyclooxygenase Inhibitors - chemistry | Antineoplastic Agents - chemistry | Matrix Metalloproteinase Inhibitors - metabolism | Matrix Metalloproteinase Inhibitors - therapeutic use | Neoplasms - drug therapy | Antineoplastic Agents - metabolism | Animals | Phosphodiesterase Inhibitors - metabolism | Thiadiazoles - chemistry | Thiadiazoles - therapeutic use | Protein Binding | Phosphodiesterase Inhibitors - chemistry | Thiadiazoles - metabolism | Carbonic Anhydrase Inhibitors - metabolism | Cyclooxygenase Inhibitors - therapeutic use | Quantitative Structure-Activity Relationship | Carbonic Anhydrase Inhibitors - therapeutic use
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 10/2014, Volume 22, Issue 19, pp. 5454 - 5465
Journal Article
FEBS Letters, ISSN 0014-5793, 09/2012, Volume 586, Issue 19, pp. 3410 - 3414
► Novel boron-containing small molecule inhibitors of phosphodiesterase 4. ► Co-crystal structure shows unique binding compared to catechol inhibitors. ► Boron... 
Cytokine inhibition | Phenoxybenzoxaborole | PDE4 | Crystal structure | phosphodiesterase 4 | NUCLEOTIDE | BIOPHYSICS | BIOCHEMISTRY & MOLECULAR BIOLOGY | ALPHA | ROFLUMILAST | SELECTIVITY | CELL BIOLOGY | Humans | Anti-Inflammatory Agents, Non-Steroidal - chemistry | Crystallography, X-Ray | Isoenzymes - chemistry | Anti-Inflammatory Agents, Non-Steroidal - pharmacology | Metals - chemistry | Isoenzymes - metabolism | Leukocytes, Mononuclear - immunology | Phosphodiesterase Inhibitors - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Binding, Competitive | Boron Compounds - chemistry | Recombinant Proteins - metabolism | Boron Compounds - pharmacology | Catalytic Domain | Recombinant Proteins - antagonists & inhibitors | Leukocytes, Mononuclear - drug effects | Isoenzymes - genetics | Bridged Bicyclo Compounds, Heterocyclic - chemistry | Models, Molecular | Phosphodiesterase Inhibitors - pharmacology | Recombinant Proteins - chemistry | Recombinant Proteins - genetics | Cyclic Nucleotide Phosphodiesterases, Type 4 - genetics | Bridged Bicyclo Compounds, Heterocyclic - pharmacology | Kinetics | In Vitro Techniques | Cytokines - biosynthesis | Isoenzymes - antagonists & inhibitors | Enzymes | Catechin | Enzyme inhibitors | Crystals | Laminated metals | Chemical properties | Structure
Journal Article
Journal Article
Nature Biotechnology, ISSN 1087-0156, 01/2010, Volume 28, Issue 1, pp. 63 - 70
Phosphodiesterase 4 (PDE4), the primary cAMP-hydrolyzing enzyme in cells, is a promising drug target for a wide range of conditions. Here we present seven... 
CAMP-SPECIFIC PHOSPHODIESTERASE | PHOSPHORYLATION | BIOTECHNOLOGY & APPLIED MICROBIOLOGY | PROTEIN-KINASE | GENE COMPOSER | SUNCUS-MURINUS | AMP-SPECIFIC PHOSPHODIESTERASE | INHIBITORS | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE | ROLIPRAM BINDING | ANTIDEPRESSANT DRUGS | Phosphodiesterase Inhibitors - therapeutic use | Phosphodiesterase Inhibitors - adverse effects | Humans | Molecular Sequence Data | Crystallography, X-Ray | Structure-Activity Relationship | Benzhydryl Compounds - chemistry | Benzhydryl Compounds - adverse effects | Phenylurea Compounds - adverse effects | Phenylurea Compounds - chemistry | Drug Design | Phosphodiesterase 4 Inhibitors | Behavior, Animal - drug effects | Biological Assay | Phosphodiesterase Inhibitors - chemistry | Benzhydryl Compounds - therapeutic use | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Disease Models, Animal | Allosteric Regulation - drug effects | Protein Structure, Tertiary | Amino Acid Sequence | Cell Line | Catalytic Domain | Models, Molecular | Phenylurea Compounds - therapeutic use | Phosphodiesterase Inhibitors - pharmacology | Vomiting - drug therapy | Cognition - drug effects | Animals | Benzhydryl Compounds - pharmacology | Mice | Phenylurea Compounds - pharmacology | Kinetics | Care and treatment | Schizophrenia | Physiological aspects | Genetic aspects | Cellular signal transduction | Cyclic adenylic acid | Research | Phosphodiesterases | Enzymes | Biotechnology | Cellular biology | Molecular biology | Cognitive ability | Crystal structure | Index Medicus
Journal Article
Medicinal Research Reviews, ISSN 0198-6325, 07/2014, Volume 34, Issue 4, pp. 703 - 743
The modulatory role of extracellular nucleotides and adenosine in relevance to purinergic cell signaling mechanisms has long been known and is an object of... 
ecto‐nucleoside triphosphate diphosphohydrolase, ecto‐nucleotide pyrophosphatase/phosphodiesterase, alkaline phosphatase | ecto‐nucleotidase | enzyme inhibitors | ecto‐5′‐nucleotidase | Ecto-nucleotidase | Enzyme inhibitors | Ecto-nucleoside triphosphate diphosphohydrolase, ecto-nucleotide pyrophosphatase/phosphodiesterase, alkaline phosphatase | Ecto-5′-nucleotidase | ecto-nucleoside triphosphate diphosphohydrolase | AUTOTAXIN INHIBITORS | CHEMISTRY, MEDICINAL | ecto-5 '-nucleotidase | CRYSTAL-STRUCTURE | MEMBRANE BOUND NTPDASES | ESCHERICHIA-COLI | ecto-nucleotidase | P-2-PURINOCEPTOR ANTAGONISTS | INTERNATIONAL UNION | LYSOPHOSPHATIDIC ACID | SELECTIVE INHIBITORS | ectonucleotide pyrophosphatase/phosphodiesterase | PHARMACOLOGY & PHARMACY | alkaline phosphatase | HUMAN PLACENTAL 5'-NUCLEOTIDASE | BULL SEMINAL PLASMA | 5'-Nucleotidase - antagonists & inhibitors | Phosphoric Diester Hydrolases - metabolism | Apyrase - antagonists & inhibitors | Humans | Alkaline Phosphatase - metabolism | Apyrase - metabolism | Enzyme Inhibitors - pharmacology | Tungsten Compounds - therapeutic use | Tungsten Compounds - pharmacology | Enzyme Inhibitors - therapeutic use | Pyrophosphatases - antagonists & inhibitors | Pyrophosphatases - metabolism | Alkaline Phosphatase - antagonists & inhibitors | Animals | Enzyme Inhibitors - chemistry | Tungsten Compounds - chemistry | 5'-Nucleotidase - metabolism
Journal Article
Journal Article