دورية أكاديمية
Mechanism of β 2 AR regulation by an intracellular positive allosteric modulator.
العنوان: | Mechanism of β |
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المؤلفون: | Liu X; Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Medicine, Tsinghua University, Beijing 100084, China., Masoudi A; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Kahsai AW; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Huang LY; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Pani B; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Staus DP; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Shim PJ; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Hirata K; Advanced Photon Technology Division, Research Infrastructure Group, SR Life Science Instrumentation Unit, RIKEN/SPring-8 Center, 1-1-1 Kouto Sayo-cho Sayo-gun, Hyogo 679-5148, Japan.; Precursory Research for Embryonic Science and Technology (PRESTO), Japan Science and Technology Agency, 4-1-8 Honcho, Kawaguchi, Saitama 332-0012, Japan., Simhal RK; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Schwalb AM; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Rambarat PK; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Ahn S; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA., Lefkowitz RJ; Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA. lefko001@receptor-biol.duke.edu kobilka@stanford.edu.; Department of Biochemistry, Duke University Medical Center, Durham, NC 27710, USA.; Howard Hughes Medical Institute, Duke University Medical Center, Durham, NC 27710, USA., Kobilka B; Beijing Advanced Innovation Center for Structural Biology, Tsinghua-Peking Joint Center for Life Sciences, School of Medicine, Tsinghua University, Beijing 100084, China. lefko001@receptor-biol.duke.edu kobilka@stanford.edu.; Department of Molecular and Cellular Physiology, Stanford University School of Medicine, 279 Campus Drive, Stanford, CA 94305, USA. |
المصدر: | Science (New York, N.Y.) [Science] 2019 Jun 28; Vol. 364 (6447), pp. 1283-1287. Date of Electronic Publication: 2019 Jun 27. |
نوع المنشور: | Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't |
اللغة: | English |
بيانات الدورية: | Publisher: American Association for the Advancement of Science Country of Publication: United States NLM ID: 0404511 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1095-9203 (Electronic) Linking ISSN: 00368075 NLM ISO Abbreviation: Science Subsets: MEDLINE |
أسماء مطبوعة: | Publication: Original Publication: New York, N.Y. : [s.n.] 1880- |
مواضيع طبية MeSH: | Adrenergic beta-2 Receptor Agonists/*chemistry , Phthalic Anhydrides/*chemistry , Receptors, Adrenergic, beta-2/*chemistry, Adrenergic beta-2 Receptor Agonists/pharmacology ; Allosteric Regulation ; Crystallography, X-Ray ; Gain of Function Mutation ; Humans ; Phthalic Anhydrides/pharmacology ; Receptors, Adrenergic, beta-2/genetics |
مستخلص: | Drugs targeting the orthosteric, primary binding site of G protein-coupled receptors are the most common therapeutics. Allosteric binding sites, elsewhere on the receptors, are less well-defined, and so less exploited clinically. We report the crystal structure of the prototypic β (Copyright © 2019 The Authors, some rights reserved; exclusive licensee American Association for the Advancement of Science. No claim to original U.S. Government Works.) |
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معلومات مُعتمدة: | U19 GM106990 United States GM NIGMS NIH HHS; R01 NS028471 United States NS NINDS NIH HHS; R01 HL016037 United States HL NHLBI NIH HHS; R37 NS028471 United States NS NINDS NIH HHS; T32 HL007101 United States HL NHLBI NIH HHS |
المشرفين على المادة: | 0 (Adrenergic beta-2 Receptor Agonists) 0 (Phthalic Anhydrides) 0 (Receptors, Adrenergic, beta-2) 1107-00-2 (2,2'-bis(3,4-dicarboxyphenyl)hexafluoropropane dianhydride) |
تواريخ الأحداث: | Date Created: 20190629 Date Completed: 20200327 Latest Revision: 20200327 |
رمز التحديث: | 20231215 |
مُعرف محوري في PubMed: | PMC6705129 |
DOI: | 10.1126/science.aaw8981 |
PMID: | 31249059 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1095-9203 |
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DOI: | 10.1126/science.aaw8981 |