ShanghaiTech University Knowledge Management System
| Structural Basis of the Diversity of Adrenergic Receptors | |
| 2019-12-03 | |
| Source Publication | CELL REPORTS
 |
| ISSN | 2211-1247 |
| Volume | 29Issue:10Pages:2929-+ |
| Status | 已发表 |
| DOI | 10.1016/j.celrep.2019.10.088 |
| Abstract | Adrenergic receptors are highly homologous while at the same time display a wide diversity of ligand and G-protein binding, and understanding this diversity is key for designing selective or biased drugs for them. Here, we determine two crystal structures of the alpha(2A) adrenergic receptor (alpha(2A)AR) in complex with a partial agonist and an antagonist. Key non-conserved residues from the ligand-binding pocket (Phe(7.39) and Tyr(6.55)) to G-protein coupling region (Ile(34.51) and Lys(34.56)) are discovered to play a key role in the interplay between partial agonism and biased signaling of alpha(2A)AR, which provides insights into the diversity of ligand binding and G-protein coupling preference of adrenergic receptors and lays the foundation for the discovery of next-generation drugs targeting these receptors. |
| URL | 查看原文 |
| Indexed By | SCI ; SCIE |
| Language | 英语 |
| Funding Project | National Key R&D Program of China[2016YFC0905900] ; National Key R&D Program of China[2018YFA0507000] ; National Key R&D Program of China[2017YFC1001300] |
| WOS Research Area | Cell Biology |
| WOS Subject | Cell Biology |
| WOS ID | WOS:000500822900001 |
| Publisher | CELL PRESS |
| WOS Keyword | CRYSTAL-STRUCTURE ; DOCKING ; AGONIST ; BINDING ; PROTEINS ; GLIDE ; MICE |
| Original Document Type | Article |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/104520 |
| Collection | 生命科学与技术学院_硕士生 iHuman研究所 iHuman研究所_特聘教授组_Andrej Sali组 iHuman研究所_特聘教授组_Raymond Stevens组 iHuman研究所_公共科研平台_IT平台 iHuman研究所_PI研究组_刘志杰组 iHuman研究所_PI研究组_陶厚朝组 iHuman研究所_PI研究组_赵素文组 iHuman研究所_PI研究组_钟桂生组 iHuman研究所_科学装置(X)_膜蛋白同步辐射线站 生命科学与技术学院_博士生 |
| Corresponding Author | Zhong, Guisheng; Wu, Dong; Zhao, Suwen |
| Affiliation | 1.ShanghaiTech Univ, iHuman Inst, Shanghai 201210, Peoples R China 2.Chinese Acad Sci, Inst Biophys, Natl Lab Biomacromol, Beijing 100101, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 5.Univ Southern Calif, Dept Biol Sci, Bridge Inst, Los Angeles, CA 90089 USA 6.Univ Southern Calif, Dept Chem, Bridge Inst, Los Angeles, CA 90089 USA |
| First Author Affilication | iHuman Institute |
| Corresponding Author Affilication | iHuman Institute; School of Life Science and Technology |
| First Signature Affilication | iHuman Institute |
| Recommended Citation GB/T 7714 | Qu, Lu,Zhou, Qingtong,Xu, Yueming,et al. Structural Basis of the Diversity of Adrenergic Receptors[J]. CELL REPORTS,2019,29(10):2929-+. |
| APA | Qu, Lu.,Zhou, Qingtong.,Xu, Yueming.,Guo, Yu.,Chen, Xiaoyu.,...&Zhao, Suwen.(2019).Structural Basis of the Diversity of Adrenergic Receptors.CELL REPORTS,29(10),2929-+. |
| MLA | Qu, Lu,et al."Structural Basis of the Diversity of Adrenergic Receptors".CELL REPORTS 29.10(2019):2929-+. |
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