دورية أكاديمية
Bitopic Binding Mode of an M 1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.
العنوان: | Bitopic Binding Mode of an M |
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المؤلفون: | Bradley SJ; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Molloy C; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Bundgaard C; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Mogg AJ; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Thompson KJ; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Dwomoh L; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Sanger HE; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Crabtree MD; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Brooke SM; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Sexton PM; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Felder CC; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Christopoulos A; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Broad LM; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.)., Tobin AB; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.) andrew.tobin@glasgow.ac.uk chris.langmead@monash.edu., Langmead CJ; The Centre for Translational Pharmacology, Institute of Molecular, Cell, and Systems Biology, College of Medical, Veterinary, and Life Sciences, University of Glasgow, Glasgow, Scotland (S.J.B., C.M., K.J.T., L.D., S.M.B., A.B.T.); Eli Lilly & Co. Neuroscience, Windlesham, Surrey, United Kingdom (C.B., A.J.M., H.E.S., M.D.C., L.M.B.); Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (P.M.S., A.C., C.J.L.); and Eli Lilly & Co. Neuroscience, Indianapolis, Indiana (C.C.F.) andrew.tobin@glasgow.ac.uk chris.langmead@monash.edu. |
المصدر: | Molecular pharmacology [Mol Pharmacol] 2018 Jun; Vol. 93 (6), pp. 645-656. Date of Electronic Publication: 2018 Apr 25. |
نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
اللغة: | English |
بيانات الدورية: | Publisher: American Society for Pharmacology and Experimental Therapeutics Country of Publication: United States NLM ID: 0035623 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1521-0111 (Electronic) Linking ISSN: 0026895X NLM ISO Abbreviation: Mol Pharmacol Subsets: MEDLINE |
أسماء مطبوعة: | Original Publication: Bethesda, MD : American Society for Pharmacology and Experimental Therapeutics |
مواضيع طبية MeSH: | Acetylcholine/*metabolism , Muscarinic Agonists/*pharmacology , Receptor, Muscarinic M1/*metabolism , Receptors, Muscarinic/*metabolism, Allosteric Regulation/drug effects ; Allosteric Site/drug effects ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Animals ; Benzimidazoles/pharmacology ; Binding Sites/drug effects ; CHO Cells ; Cell Line ; Clinical Trials as Topic ; Cricetinae ; Cricetulus ; Humans ; Learning/drug effects ; Male ; Memory/drug effects ; Mice ; Mice, Inbred C57BL ; Protein Binding/drug effects ; Rats ; Rats, Wistar |
مستخلص: | The realization of the therapeutic potential of targeting the M (Copyright © 2018 by The Author(s).) |
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معلومات مُعتمدة: | United Kingdom Wellcome Trust; 201529/Z/16/Z United Kingdom Wellcome Trust; MR/P019366/1 United Kingdom Medical Research Council; C596/A17196 United Kingdom Cancer Research UK |
المشرفين على المادة: | 0 (Benzimidazoles) 0 (GSK 1034702) 0 (Muscarinic Agonists) 0 (Receptor, Muscarinic M1) 0 (Receptors, Muscarinic) 43135-91-7 (benzimidazol-2-one) N9YNS0M02X (Acetylcholine) |
تواريخ الأحداث: | Date Created: 20180427 Date Completed: 20190201 Latest Revision: 20190201 |
رمز التحديث: | 20231215 |
مُعرف محوري في PubMed: | PMC5963591 |
DOI: | 10.1124/mol.118.111872 |
PMID: | 29695609 |
قاعدة البيانات: | MEDLINE |
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