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1Efficient and Highly Scalable Mechanistic Characterization of Ion Channel Function in Drug Discovery
المؤلفون: Renee Emkey, Tianbo Li, Martin Ginkel, Stephan Heyse, Leigh Foster, Jun Chen, Ada Yee, Stephan Steigele
المصدر: Biophysical Journal. 118:579a
مصطلحات موضوعية: Drug discovery, Chemistry, Scalability, Biophysics, Computational biology, Function (biology), Ion channel, Characterization (materials science)
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2Development of Novel Dual Binders as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors
المؤلفون: Zihao Hua, Bryan Egge, Erin L. Mullady, Hakan Gunaydin, John L. Buchanan, Steve Schneider, Xin Huang, Yohannes Teffera, Renee Emkey, Howard Bregman, Randy Serafino, Mary K. Stanton, Erin F. DiMauro, Jingzhou Liu, Virginia Berry, Douglas Saffran, Angel Guzman-Perez, Jennifer Dovey, Liyue Huang, Craig A. Strathdee, Susan M. Turci, Yan Gu, Paul S. Andrews, John Newcomb, Cindy Wilson, Ankita Mishra, Lisa Acquaviva, Nagasree Chakka
المصدر: Journal of Medicinal Chemistry. 56:10003-10015
مصطلحات موضوعية: Models, Molecular, Tankyrases, Dose-Response Relationship, Drug, Molecular Structure, biology, Chemistry, Drug discovery, Poly ADP ribose polymerase, Wnt signaling pathway, Administration, Oral, Biological Availability, Structure-Activity Relationship, Biochemistry, Drug Discovery, biology.protein, Humans, Molecular Medicine, Structure–activity relationship, Enzyme Inhibitors, Pharmacophore, Axin Protein, Polymerase
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3
المؤلفون: Jeffrey R. Simard, Violeta Yu, Matthew H. Plant, Renee Emkey
المصدر: ASSAY and Drug Development Technologies. 11:152-162
مصطلحات موضوعية: Methyltransferase, Repressor, macromolecular substances, Buffers, Methylation, Antibodies, Histone H3, Fluorescence Polarization Immunoassay, Drug Discovery, Humans, Enhancer of Zeste Homolog 2 Protein, Enzyme Inhibitors, biology, EZH2, Polycomb Repressive Complex 2, Reproducibility of Results, Reference Standards, Molecular biology, Recombinant Proteins, High-Throughput Screening Assays, Biochemistry, Data Interpretation, Statistical, Histone methyltransferase, Biotinylation, biology.protein, Molecular Medicine, Indicators and Reagents, Streptavidin, Peptides, PRC2, Algorithms
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4
المؤلفون: Fredrik Pehr Marmsater, Jeffrey M. Schkeryantz, Dana Rae Benesh, Maria-Jesus Blanco, Amy Clemens-Smith, Renee Emkey, Kirk W. Johnson, Michael P. Johnson, Fese Mokube, Groendyke Todd Michael, James Allen Knobelsdorf, Tony Pisal Tang, Mark A. Muhlhauser, Cortez Guillermo S, Thomas Daniel Aicher, Albert Khilevich, Steven Swanson, John T. Catlow
المصدر: Bioorganicmedicinal chemistry letters. 27(2)
مصطلحات موضوعية: 0301 basic medicine, Migraine Disorders, Clinical Biochemistry, Allosteric regulation, Pharmaceutical Science, Pharmacology, Receptors, Metabotropic Glutamate, Biochemistry, 03 medical and health sciences, Structure-Activity Relationship, 0302 clinical medicine, Dogs, Allosteric Regulation, Drug Discovery, Animals, Humans, Molecular Biology, Receptors, Leukotriene, Sulfonamides, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, Metabotropic glutamate receptor 5, Organic Chemistry, Potentiator, Rats, Cysteinyl leukotriene receptor 1, 030104 developmental biology, Metabotropic receptor, Metabotropic glutamate receptor, Molecular Medicine, Metabotropic glutamate receptor 1, Metabotropic glutamate receptor 2, 030217 neurology & neurosurgery
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5
المؤلفون: Junliang Hao, Wesley H. Anderson, Cohen Michael Philip, Kjell A. Svensson, Michael A. Statnick, Donald R. Gehlert, Joseph H. Krushinski, Hellman Sarah Lynne, Michelle M Menezes, Jeffrey W Cramer, Julie F. Falcone, Xushan Wang, Rebecca A. Wright, John Mehnert Schaus, Neil W. DeLapp, Reinhard Matthew Robert, S Michelle Morin, Charles R. Yang, Todd R. Wiernicki, Ilya Okun, Renee Emkey, Benjamin L. Adams, Beverly A. Heinz, Brian G. Getman, James P. Beck, Robert F. Bruns, Virginia L. Lucaites, Todd M. Suter, Deanna L Maren, David L. Nelson, Kelly L. Knopp, Borys V. Rogovoy
المصدر: The Journal of Pharmacology and Experimental Therapeutics
مصطلحات موضوعية: 0301 basic medicine, Agonist, Male, medicine.drug_class, Allosteric regulation, Adamantane, Pharmacology, Biology, Tachyphylaxis, Dihydrexidine, 03 medical and health sciences, Mice, 0302 clinical medicine, Dopamine receptor D1, Neuropharmacology, Allosteric Regulation, Dopamine, medicine, Animals, Humans, Benzopyrans, Gene Knock-In Techniques, Behavior, Animal, Dose-Response Relationship, Drug, Receptors, Dopamine D1, Potentiator, Isoquinolines, Stereotypy (non-human), Protein Transport, 030104 developmental biology, HEK293 Cells, Molecular Medicine, Female, 030217 neurology & neurosurgery, Locomotion, medicine.drug
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6
المؤلفون: Beth D. Youngblood, Alessandro Boezio, Stephanie D. Geuns-Meyer, Maosheng Zhang, Angel Guzman-Perez, Laurie B. Schenkel, Yohannes Teffera, Weiya Wang, Philip R. Olivieri, Renee Emkey, Hakan Gunaydin, Josie H. Lee, Holly L. Deak, Violeta Yu, Russell Graceffa, Sonya G. Lehto, Narender R. Gavva
المصدر: Journal of medicinal chemistry. 59(6)
مصطلحات موضوعية: 0301 basic medicine, Models, Molecular, Biological Transport, Active, Nerve Tissue Proteins, CHO Cells, Pharmacology, In Vitro Techniques, Madin Darby Canine Kidney Cells, 03 medical and health sciences, Transient receptor potential channel, chemistry.chemical_compound, Structure-Activity Relationship, 0302 clinical medicine, Cricetulus, Dogs, Transient Receptor Potential Channels, Pharmacokinetics, In vivo, Drug Discovery, Potency, Animals, Humans, IC50, Quinazolinone, TRPA1 Cation Channel, Pain Measurement, Oxadiazoles, Dose-Response Relationship, Drug, Antagonist, food and beverages, Small molecule, High-Throughput Screening Assays, Rats, 030104 developmental biology, chemistry, Purines, Microsomes, Liver, Quinazolines, Molecular Medicine, Calcium Channels, psychological phenomena and processes, 030217 neurology & neurosurgery
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7
المؤلفون: Hao Chen, Linda F. Epstein, Douglas A. Whittington, Renee Emkey
المصدر: Journal of Biological Chemistry. 287:37447-37457
مصطلحات موضوعية: Models, Molecular, Pyridines, Amino Acid Motifs, Receptor Protein-Tyrosine Kinases, Mutation, Missense, Spodoptera, Crystallography, X-Ray, medicine.disease_cause, Binding, Competitive, Biochemistry, Receptor tyrosine kinase, Cell Line, Neuroblastoma, Adenosine Triphosphate, Crizotinib, immune system diseases, Catalytic Domain, hemic and lymphatic diseases, medicine, Animals, Humans, Anaplastic lymphoma kinase, Anaplastic Lymphoma Kinase, Kinase activity, Molecular Biology, Benzoxazoles, Mutation, biology, Chemistry, Point mutation, Hydrogen Bonding, Cell Biology, Molecular biology, Protein kinase domain, Structural Homology, Protein, Proteolysis, Protein Structure and Folding, Cancer research, biology.protein, Pyrazoles, Protein Binding, medicine.drug
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8
المؤلفون: Peter Yakowec, Jin Tang, Violeta Yu, Alexander M. Long, Ralf Schwandner, Tanja Fisch, Josie Han Lee, Renee Emkey, Markus Hierl, Hao Chen
المصدر: SLAS Discovery. 17:27-38
مصطلحات موضوعية: Jumonji Domain-Containing Histone Demethylases, Molecular Sequence Data, Lysine, Methylation, Biochemistry, Analytical Chemistry, Histone H3, High-Throughput Screening Assays, Fluorescence Resonance Energy Transfer, Amino Acid Sequence, Enzyme Inhibitors, Peptide sequence, Demethylation, Histone Demethylases, Immunoassay, biology, biology.protein, Molecular Medicine, Demethylase, Peptides, Biotechnology
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9
المؤلفون: Evelyn Yang, Hao Chen, Mark Michaels, Jin Tang, Steve Schneider, Renee Emkey, Paul S. Andrews
المصدر: ASSAY and Drug Development Technologies. 8:471-487
مصطلحات موضوعية: HECT domain, RHOA, Ubiquitin-Protein Ligases, Protein Array Analysis, Ubiquitin-Activating Enzymes, Biological pathway, Ubiquitin, Transforming Growth Factor beta, Drug Discovery, Humans, chemistry.chemical_classification, DNA ligase, biology, Ubiquitination, Recombinant Proteins, Ubiquitin ligase, Cell biology, Proteasome, Biochemistry, chemistry, Bone Morphogenetic Proteins, biology.protein, Protein microarray, Molecular Medicine, Signal Transduction
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10
المؤلفون: Ryan White, Erin F. DiMauro, Stephen Hitchcock, Robert T. Fremeau, Ming Y. Huang, Isaac E. Marx, Jason Brooks Human, Liyue Huang, Josie H. Lee, Alan C. Cheng, Vinod F. Patel, Xingwen Li, Matthew W. Martin, Renee Emkey
المصدر: Bioorganic & Medicinal Chemistry Letters. 19:31-35
مصطلحات موضوعية: Chemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, Amides, Biochemistry, Rats, Receptor, Cannabinoid, CB2, Structure-Activity Relationship, Pharmacokinetics, Drug Discovery, Microsomes, Liver, Animals, Humans, Molecular Medicine, Sulfones, Molecular Biology
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11
المؤلفون: Ryan White, James Brown, Jean-Christophe Harmange, Xiaoyang Xia, Josie Han Lee, Yuan Cheng, Robert T. Fremeau, Beth J. Hoffman, Susan A. Tomlinson, Matthew W. Martin, Liyue Huang, Erin F. DiMauro, Stephen Hitchcock, Hung Q. Nguyen, John L. Buchanan, Vinod F. Patel, Ming Huang, William H. Buckner, Brian K. Albrecht, Fen-Fen Lin, Renee Emkey
المصدر: Journal of Medicinal Chemistry. 51:5019-5034
مصطلحات موضوعية: Models, Molecular, Agonist, Stereochemistry, medicine.drug_class, medicine.medical_treatment, Drug Evaluation, Preclinical, Administration, Oral, Biological Availability, Oxadiazole, CHO Cells, Receptor, Cannabinoid, CB2, Structure-Activity Relationship, chemistry.chemical_compound, Cricetulus, Cricetinae, Drug Discovery, Cannabinoid receptor type 2, medicine, Animals, Humans, Structure–activity relationship, Oxadiazoles, Virtual screening, Chemistry, Combinatorial chemistry, Rats, Bioavailability, Aminoquinolines, Molecular Medicine, lipids (amino acids, peptides, and proteins), Cannabinoid, Pharmacophore
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12
المؤلفون: Sean P. Hollinshead, Emanuele Sher, Kathy H. Pearson, Ruud Zwart, Gordon I. McPhie, Lisa M. Broad, Martin Lee, Dell Colin Peter, S. Richard Baker, Renee Emkey, Louise Wallace
المصدر: Journal of Pharmacology and Experimental Therapeutics. 318:1108-1117
مصطلحات موضوعية: Agonist, Pyridines, medicine.drug_class, Receptors, Nicotinic, Pharmacology, Cell Line, Xenopus laevis, Ganglion type nicotinic receptor, Muscarinic acetylcholine receptor, medicine, Animals, Humans, Nicotinic Agonists, Acetylcholine receptor, Galantamine, Chemistry, Drug Synergism, Bridged Bicyclo Compounds, Heterocyclic, Recombinant Proteins, Protein Subunits, Nicotinic acetylcholine receptor, Nicotinic agonist, Biochemistry, Epibatidine, Molecular Medicine, Alpha-4 beta-2 nicotinic receptor, medicine.drug
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13
المؤلفون: Renee Emkey, Martin Smith, Jesus A. Gutierrez, Carolyn A. Cook, Tracy L. Borts, Christina J. Wiggins
المصدر: Journal of Neurochemistry. 86:255-266
مصطلحات موضوعية: Agonist, medicine.medical_specialty, medicine.drug_class, Biology, Biochemistry, Cell biology, Cellular and Molecular Neuroscience, chemistry.chemical_compound, Metabotropic receptor, Endocrinology, chemistry, Internal medicine, medicine, Serotonin, Signal transduction, Neurotransmitter, Receptor, 5-HT receptor, G protein-coupled receptor
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14Novel and Selective Small Molecule Stimulators of Osteoprotegerin Expression Inhibit Bone Resorption
المؤلفون: Tina Fuson, Srinivasan Chandrasekhar, Rebecca R. Miles, Renee Emkey, David L. Halladay, Rachelle J. Sells Galvin, Yanping Xu, Ricky L. Cain, Henry Uhlman Bryant, T. John Martin, Kannan Thirunavukkarasu, Yanfei L. Ma, Qing Qiang Zeng, Jude E. Onyia, Xuhao Yang
المصدر: Journal of Pharmacology and Experimental Therapeutics. 309:369-379
مصطلحات موضوعية: Male, musculoskeletal diseases, medicine.medical_specialty, Stromal cell, Pyridines, Cellular differentiation, Anti-Inflammatory Agents, Osteoclasts, Receptors, Cytoplasmic and Nuclear, Receptors, Tumor Necrosis Factor, Bone resorption, Rats, Sprague-Dawley, Mice, Structure-Activity Relationship, Paracrine signalling, Osteoprotegerin, Osteoclast, Internal medicine, Tumor Cells, Cultured, medicine, Animals, Humans, Bone Resorption, Promoter Regions, Genetic, Receptor, Glycoproteins, Pharmacology, Chemistry, Cell Differentiation, Rats, Disease Models, Animal, Endocrinology, medicine.anatomical_structure, Gene Expression Regulation, Benzamides, Molecular Medicine, Female, Tumor necrosis factor alpha
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15
المؤلفون: Renee Emkey, C. Ronald Kahn
المصدر: Comprehensive Physiology
مصطلحات موضوعية: medicine.medical_specialty, Insulin, medicine.medical_treatment, GRB10, Biology, IRS2, IRS1, Insulin receptor, Endocrinology, Downregulation and upregulation, Internal medicine, Insulin receptor substrate, medicine, biology.protein, Insulin-like growth factor 1 receptor
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16
المؤلفون: Bentley Cheatham, Renee Emkey, G Inoue, C R Kahn
المصدر: Journal of Biological Chemistry. 273:11548-11555
مصطلحات موضوعية: medicine.medical_specialty, Insulin Receptor Substrate Proteins, Insulin, medicine.medical_treatment, Tyrosine phosphorylation, Cell Biology, Biology, Biochemistry, Cell biology, Cytosol, chemistry.chemical_compound, Insulin receptor, Endocrinology, chemistry, Insulin receptor substrate, Internal medicine, medicine, biology.protein, Phosphorylation, Phosphatidylinositol, Molecular Biology
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17
المؤلفون: C. Ronald Kahn, Renee Emkey
المصدر: Journal of Biological Chemistry. 272:31182-31189
مصطلحات موضوعية: biology, Tyrosine phosphorylation, Cell Biology, Protein tyrosine phosphatase, Biochemistry, Receptor tyrosine kinase, Cell biology, chemistry.chemical_compound, Insulin receptor, chemistry, ErbB, Phorbol, biology.protein, Phosphorylation, Molecular Biology, Tyrosine kinase
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18
المؤلفون: Patricia Merkel, Richard T. Lewis, Violeta Yu, Allison Drew, Steven Szilvassy, Karina Romero, Renee Emkey, Hao Chen, Douglas Saffran, Rachael L. Brake, Yohannes Teffera, Christiane Bode, Paul S. Andrews, Man Xu, Earl Moore, Deborah Choquette, John Stellwagen, Linda F. Epstein, Michele Potashman, Douglas A. Whittington
المصدر: Journal of medicinal chemistry. 55(14)
مصطلحات موضوعية: Models, Molecular, Administration, Oral, Biological Availability, Antineoplastic Agents, Pharmacology, Substrate Specificity, Inhibitory Concentration 50, Drug Stability, hemic and lymphatic diseases, Cell Line, Tumor, Drug Discovery, Tumor regression, medicine, Potency, Anaplastic lymphoma kinase, Animals, Humans, Anaplastic Lymphoma Kinase, Protein Kinase Inhibitors, Chemistry, Kinase, Imidazoles, Cancer, Receptor Protein-Tyrosine Kinases, Metabolic stability, medicine.disease, Bioavailability, Protein Structure, Tertiary, Rats, Microsomes, Liver, Molecular Medicine, Structure based
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19
المؤلفون: Bee-Chun Sun, Renee Emkey, Ivonne Archibeque, Laurie B. Schenkel, Liqin Liu, Josie Han Lee, Violeta Yu, Stephanie D. Geuns-Meyer, Jeanne Pistillo
المصدر: Experimental hematology. 41(5)
مصطلحات موضوعية: Cancer Research, Oncogene Proteins, Fusion, Cell, Biology, Cell Line, hemic and lymphatic diseases, Genetics, medicine, STAT5 Transcription Factor, Animals, Humans, Phosphorylation, Molecular Biology, Protein Kinase Inhibitors, Cells, Cultured, Cell Proliferation, chemistry.chemical_classification, Dose-Response Relationship, Drug, Cell growth, Precursor Cells, B-Lymphoid, Reproducibility of Results, Cell Biology, Hematology, Janus Kinase 2, Molecular biology, Small molecule, Enzyme assay, High-Throughput Screening Assays, Enzyme, medicine.anatomical_structure, chemistry, Biochemistry, Cell culture, Tyrosine kinase 2, biology.protein, Leukocytes, Mononuclear, Janus kinase
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20
المؤلفون: Richard T. Lewis, Douglas A. Whittington, James R. Falsey, Rachael L. Brake, Elizabeth M. Doherty, Renee Emkey, Alan C. Cheng, Marian C. Bryan
المصدر: Journal of medicinal chemistry. 55(4)
مصطلحات موضوعية: Models, Molecular, Stereochemistry, medicine.drug_class, Protein Conformation, High-throughput screening, Carboxamide, Antineoplastic Agents, Crystallography, X-Ray, Receptor, IGF Type 1, chemistry.chemical_compound, Structure-Activity Relationship, Piperidines, hemic and lymphatic diseases, Cell Line, Tumor, Drug Discovery, medicine, Fluorescence Resonance Energy Transfer, Anaplastic lymphoma kinase, Humans, Anaplastic Lymphoma Kinase, IC50, Insulin-like growth factor 1 receptor, Molecular Structure, Kinase, Chemistry, Receptor Protein-Tyrosine Kinases, Stereoisomerism, Amides, High-Throughput Screening Assays, body regions, Pyrimidines, Protein kinase domain, Biochemistry, Molecular Medicine, Piperidine, Hydrophobic and Hydrophilic Interactions