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1Development 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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2
المؤلفون: Angel Guzman-Perez, Erin L. Mullady, Randy Serafino, Erin F. DiMauro, Hakan Gunaydin, Xin Huang, Liyue Huang, Jingzhou Liu, Virginia Berry, Bryan Egge, Nagasree Chakka, Cindy Wilson, Steve Schneider, John Newcomb, Yan Gu, Yohannes Teffera, Susan M. Turci, Ankita Mishra, Paul S. Andrews, Howard Bregman, Craig A. Strathdee
المصدر: Journal of Medicinal Chemistry. 56:4320-4342
مصطلحات موضوعية: Models, Molecular, Molecular model, Poly ADP ribose polymerase, Administration, Oral, Biological Availability, In Vitro Techniques, Pharmacology, medicine.disease_cause, Mice, Structure-Activity Relationship, Pharmacokinetics, Transcription (biology), Drug Discovery, medicine, Animals, Axin Protein, Oxazolidinones, Tankyrases, Binding Sites, Oncogene, Chemistry, Stereoisomerism, Rats, Bioavailability, Biochemistry, Microsomes, Liver, Molecular Medicine, Benzimidazoles, Carcinogenesis
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3
المؤلفون: Xin Huang, Susan M. Turci, Zihao Hua, Randy Serafino, Liyue Huang, Jin Tang, Jason Brooks Human, Ryan White, Lisa Acquaviva, Jennifer Dovey, Barbara Grubinska, Oleg Epstein, Doug Saffran, Huilin Zhao, Steve Schneider, Howard Bregman, Hongbing Huang, Anne B. O’Connor, Violeta Yu, John Newcomb, Jonathan T. Goldstein, Nagasree Chakka, Matthew W. Martin, Vinod F. Patel, Craig A. Strathdee, Virginia Berry, Alexander M. Long, Cindy Wilson, Erin F. DiMauro, Hakan Gunaydin
المصدر: ACS Medicinal Chemistry Letters. 3:1059-1064
مصطلحات موضوعية: Gene isoform, chemistry.chemical_classification, business.industry, Organic Chemistry, Wnt signaling pathway, LRP6, Pharmacology, Biochemistry, Enzyme, chemistry, Drug Discovery, Cancer research, Medicine, Phosphorylation, Casein kinase 1, Signal transduction, business, Cell potency
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4
المؤلفون: Natesan Murugesan, Zhengxiang Gu, Philip D. Stein, Sharon Bisaha, Steve Spergel, Ravi Girotra, Ving G. Lee, John Lloyd, Raj N. Misra, Joan Schmidt, Arvind Mathur, Leslie Stratton, Yolanda F. Kelly, Eileen Bird, Tom Waldron, Eddie C.-K. Liu, Rongan Zhang, Helen Lee, Randy Serafino, Benoni Abboa-Offei, Parker Mathers, Mary Giancarli, Andrea Ann Seymour, Maria L. Webb, Suzanne Moreland, Joel C. Barrish, John T. Hunt
المصدر: Journal of Medicinal Chemistry. 41:5198-5218
مصطلحات موضوعية: chemistry.chemical_classification, Biphenyl, Endothelin Antagonists, Chemistry, Stereochemistry, Substituent, Antagonist, Sulfonamide, chemistry.chemical_compound, Orally active, In vivo, Drug Discovery, Molecular Medicine, Endothelin receptor
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5
المؤلفون: Virginia Berry, Steve Schneider, Liyue Huang, Doug Saffran, Cindy Wilson, Randy Serafino, Angel Guzman-Perez, Lisa Acquaviva, Hongbing Huang, Erin F. DiMauro, Hakan Gunaydin, Howard Bregman, Jennifer Dovey, Xin Huang
المصدر: ACS medicinal chemistry letters. 4(12)
مصطلحات موضوعية: Gene isoform, chemistry.chemical_classification, Nicotinamide, Poly ADP ribose polymerase, Organic Chemistry, Mutant, Wnt signaling pathway, Cancer, Biology, medicine.disease, Biochemistry, chemistry.chemical_compound, Enzyme, chemistry, Drug Discovery, medicine, Cell potency
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6
المؤلفون: R.B. Cohen, Kenneth E.J. Dickinson, Zhengxiang Gu, S. Skwish, Michael A. Poss, Randy Serafino, James R. Powell, Carol L. Delaney, Suzanne Moreland, Denis E. Ryono
المصدر: British Journal of Pharmacology. 113:179-189
مصطلحات موضوعية: Male, Angiotensin receptor, medicine.medical_specialty, medicine.drug_class, Tetrazoles, In Vitro Techniques, Phosphatidylinositols, Losartan, Muscle, Smooth, Vascular, Angiotensin Receptor Antagonists, Internal medicine, medicine, Animals, Receptor, Antihypertensive Agents, Pharmacology, Membranes, Chemistry, Angiotensin II, Biphenyl Compounds, Rasm, Imidazoles, Receptor antagonist, Rats, Biphenyl compound, Endocrinology, Competitive antagonist, Adrenal Cortex, cardiovascular system, Rabbits, Angiotensin I, Extracellular Space, hormones, hormone substitutes, and hormone antagonists, Research Article, Muscle Contraction, medicine.drug
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7
المؤلفون: Suzanne Moreland, Kenneth E.J. Dickinson, Arthur V. Miller, Randy Serafino, Carol L. Delaney, Harold N. Weller, S. A. Hedberg
المصدر: ChemInform. 24
مصطلحات موضوعية: chemistry.chemical_classification, Angiotensin II receptor type 1, Chemistry, Stereochemistry, General Medicine, Combinatorial chemistry, Angiotensin II, Alkyl
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8
المؤلفون: Carol L. Delaney, Robert Cohen, Hossain Monshizadegan, Eddie C.-K. Liu, Suzanne Moreland, Kenneth E.J. Dickinson, Maria L. Webb, Randy Serafino
المصدر: Biochemical and Biophysical Research Communications. 185:887-892
مصطلحات موضوعية: Angiotensin receptor, medicine.medical_specialty, Vascular smooth muscle, Inositol Phosphates, Biophysics, Aorta, Thoracic, Receptors, Cell Surface, In Vitro Techniques, Biology, Transfection, Peptides, Cyclic, Biochemistry, Muscle, Smooth, Vascular, Cell Line, Potassium Chloride, Norepinephrine, chemistry.chemical_compound, Cerebellum, Internal medicine, medicine, Animals, Inositol, Cloning, Molecular, Molecular Biology, Cells, Cultured, BQ-123, Angiotensin II receptor type 1, Receptors, Endothelin, Endothelin receptor antagonist, Angiotensin II, Endothelins, Cell Membrane, Cell Biology, Recombinant Proteins, Kinetics, Endocrinology, chemistry, cardiovascular system, Rabbits, Endothelin receptor, Muscle Contraction
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9
المؤلفون: Christopher J. Molloy, Maria L. Webb, Hossain Monshizadegan, Robert Cohen, Elizabeth A. Bogosian, Suzanne Moreland, Randy Serafino, Kenneth E.J. Dickinson, T.J. Murphy, Eddie C.-K. Liu, Anders Hedberg
المصدر: Peptides. 13:499-508
مصطلحات موضوعية: Sarcosine, Physiology, Population, Adrenal Gland Neoplasms, DNA, Single-Stranded, Pheochromocytoma, Biology, Phosphatidylinositols, Biochemistry, Angiotensin Receptor Antagonists, Cellular and Molecular Neuroscience, chemistry.chemical_compound, Endocrinology, Cyclic AMP, Tumor Cells, Cultured, Animals, RNA, Messenger, Phosphorylation, Binding site, Receptor, education, Cyclic GMP, education.field_of_study, Arachidonic Acid, Receptors, Angiotensin, Angiotensin II, Cell Membrane, Nucleic Acid Hybridization, Proteins, Molecular biology, Rats, Dissociation constant, chemistry, Calcium, Signal transduction, hormones, hormone substitutes, and hormone antagonists, Signal Transduction
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10
المؤلفون: Sundeep Dugar, Nyeemah Grazier, Brian J. Gavin, Jack Z. Gougoutas, Mark S. Kirby, Karnail S. Atwal, Kenneth J. Yost, Saleem Ahmad, John D. Dimarco, Lidia M. Doweyko, Bang-Chi Chen, Khehyong Ngu, Charles R. Dorso, Randy Serafino, Shung C. Wu, Alice Y. Chen, Shih-Jung Lan
المصدر: Journal of medicinal chemistry. 44(20)
مصطلحات موضوعية: Cyclopropanes, Sodium-Hydrogen Exchangers, Stereochemistry, Sodium, chemistry.chemical_element, Administration, Oral, Biological Availability, Stereoisomerism, Crystallography, X-Ray, Chemical synthesis, Guanidines, Cyclopropane, Cell Line, chemistry.chemical_compound, Structure-Activity Relationship, Cricetinae, Drug Discovery, Structure–activity relationship, Animals, Humans, Protein Isoforms, Cation Transport Proteins, Sodium-Hydrogen Exchanger 1, Cariporide, Aryl, Membrane Proteins, Rats, chemistry, Molecular Medicine, Selectivity
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11
المؤلفون: Randy Serafino, H Weber, Suzanne Moreland, J Norman, Maria L. Webb, David S. Taylor, Christopher J. Molloy
المصدر: Molecular endocrinology (Baltimore, Md.). 8(2)
مصطلحات موضوعية: medicine.medical_specialty, Time Factors, Mitosis, Biology, Models, Biological, Muscle, Smooth, Vascular, chemistry.chemical_compound, Endocrinology, Internal medicine, medicine, Animals, Phosphorylation, Receptor, Molecular Biology, Cells, Cultured, Receptors, Angiotensin, DNA synthesis, Receptors, Endothelin, Angiotensin II, Endothelins, Rasm, Tyrosine phosphorylation, General Medicine, DNA, Endothelin 1, Rats, chemistry, cardiovascular system, Calcium, Signal transduction, Protein Kinases, hormones, hormone substitutes, and hormone antagonists, circulatory and respiratory physiology, Signal Transduction
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12
المؤلفون: Philip D. Stein, Anders Hedberg, Eddie C.-K. Liu, David M. Floyd, Maria L. Webb, Sesha Natarajan, Stephen M. Festin, John T. Hunt, Rongan Zhang, Carol L. Delaney, Ving G. Lee, Randy Serafino, Diane M. McMullen, Mark S. Bolgar, Suzanne Moreland
المصدر: Bioorganicmedicinal chemistry. 1(1)
مصطلحات موضوعية: Endothelin Receptor Antagonists, Endothelin receptor type A, Stereochemistry, Clinical Biochemistry, Guinea Pigs, Molecular Sequence Data, Pharmaceutical Science, Peptide, Biochemistry, Partial agonist, Muscle, Smooth, Vascular, Receptor subtype, Radioligand Assay, Structure-Activity Relationship, Drug Discovery, Animals, Amino Acid Sequence, Receptor, Molecular Biology, chemistry.chemical_classification, Bicyclic molecule, Endothelin-1, Chemistry, Receptors, Endothelin, Endothelins, Organic Chemistry, Antagonist, Receptor, Endothelin A, Rats, Carotid Arteries, Vasoconstriction, cardiovascular system, Molecular Medicine, Rabbits, Endothelin receptor
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13
المؤلفون: Inge M. Michel, Kenneth E.J. Dickinson, Hossain Monshizadegan, Suzanne Moreland, Maria L. Webb, T.J. Murphy, Randy Serafino, Steven M. Seiler
المصدر: Regulatory peptides. 44(2)
مصطلحات موضوعية: Physiology, Pyridines, Clinical Biochemistry, Tetrazoles, CHO Cells, Biology, 1-Sarcosine-8-Isoleucine Angiotensin II, Transfection, Biochemistry, Losartan, Cellular and Molecular Neuroscience, Angiotensin Receptor Antagonists, Radioligand Assay, Endocrinology, Cricetinae, medicine, Animals, Binding site, Cloning, Molecular, Receptor, Angiotensin II receptor type 1, Binding Sites, Receptors, Angiotensin, Chinese hamster ovary cell, Angiotensin II, Biphenyl Compounds, Imidazoles, DNA, Molecular biology, Calcium, Signal transduction, Angiotensin I, Cyclase activity, hormones, hormone substitutes, and hormone antagonists, medicine.drug, Adenylyl Cyclases, Signal Transduction