دورية أكاديمية
Small-Molecule Positive Allosteric Modulators of the β 2 -Adrenoceptor Isolated from DNA-Encoded Libraries.
العنوان: | Small-Molecule Positive Allosteric Modulators of the β |
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المؤلفون: | Ahn S; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Pani B; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Kahsai AW; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Olsen EK; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Husemoen G; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Vestergaard M; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Jin L; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Zhao S; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Wingler LM; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Rambarat PK; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Simhal RK; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Xu TT; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Sun LD; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Shim PJ; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Staus DP; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Huang LY; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Franch T; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Chen X; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.)., Lefkowitz RJ; Departments of Medicine (S.A., B.P., A.W.K., L.M.W., P.K.R., R.K.S., T.T.X., L.D.S., D.P.S., L.-Y.H., R.J.L.) and Biochemistry (R.J.L.) and Howard Hughes Medical Institute (L.M.W., D.P.S., R.J.L.), Duke University Medical Center, Durham, North Carolina; Nuevolution A/S, Copenhagen, Denmark (E.K.O., G.H., M.V., T.F.); Department of Medicinal Chemistry, School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu, China (L.J., S.Z., X.C.); and Department of Biology, Duke University, Durham, North Carolina (P.J.S.) lefko001@receptor-biol.duke.edu. |
المصدر: | Molecular pharmacology [Mol Pharmacol] 2018 Aug; Vol. 94 (2), pp. 850-861. Date of Electronic Publication: 2018 May 16. |
نوع المنشور: | Journal Article; Research Support, N.I.H., Extramural; 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: | Adrenergic beta-2 Receptor Agonists/*metabolism , Receptors, Adrenergic, beta-2/*chemistry , Receptors, Adrenergic, beta-2/*metabolism , Small Molecule Libraries/*pharmacology, Allosteric Regulation/drug effects ; Allosteric Site/drug effects ; Drug Synergism ; GTP-Binding Proteins/metabolism ; Gene Library ; Molecular Structure ; Small Molecule Libraries/chemistry ; Structure-Activity Relationship ; Substrate Specificity ; beta-Arrestin 1/metabolism |
مستخلص: | Conventional drug discovery efforts at the β Competing Interests: The authors declare no conflict of interest. (Copyright © 2018 by The Author(s).) |
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معلومات مُعتمدة: | R01 HL016037 United States HL NHLBI NIH HHS; T32 HL007101 United States HL NHLBI NIH HHS; United States HHMI Howard Hughes Medical Institute |
المشرفين على المادة: | 0 (Adrenergic beta-2 Receptor Agonists) 0 (Receptors, Adrenergic, beta-2) 0 (Small Molecule Libraries) 0 (beta-Arrestin 1) EC 3.6.1.- (GTP-Binding Proteins) |
تواريخ الأحداث: | Date Created: 20180518 Date Completed: 20190322 Latest Revision: 20190322 |
رمز التحديث: | 20221213 |
مُعرف محوري في PubMed: | PMC6022804 |
DOI: | 10.1124/mol.118.111948 |
PMID: | 29769246 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1521-0111 |
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DOI: | 10.1124/mol.118.111948 |