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Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy

文献类型：期刊论文

作者Duan, Jia2,3; Shen, Dan-dan1,5; Zhou, X. Edward6; Bi, Peng1,5; Liu, Qiu-feng2; Tan, Yang-xia2,3,4; Zhuang, You-wen2,3; Zhang, Hui-bing1,5; Xu, Pei-yu2,3; Huang, Si-Jie2,3,4
刊名NATURE COMMUNICATIONS
出版日期2020-08-17
卷号11期号:1页码:10
ISSN号2041-1723
DOI10.1038/s41467-020-17933-8
通讯作者Zhang, Yan(zhang_yan@zju.edu.cn) ; Xu, H. Eric(eric.xu@simm.ac.cn) ; Jiang, Yi(yijiang@simm.ac.cn)
英文摘要Vasoactive intestinal polypeptide receptor (VIP1R) is a widely expressed class B G protein-coupled receptor and a drug target for the treatment of neuronal, metabolic, and inflammatory diseases. However, our understanding of its mechanism of action and the potential of drug discovery targeting this receptor is limited by the lack of structural information of VIP1R. Here we report a cryo-electron microscopy structure of human VIP1R bound to PACAP27 and Gs heterotrimer, whose complex assembly is stabilized by a NanoBiT tethering strategy. Comparison with other class B GPCR structures reveals that PACAP27 engages VIP1R with its N-terminus inserting into the ligand binding pocket at the transmembrane bundle of the receptor, which subsequently couples to the G protein in a receptor-specific manner. This structure has provided insights into the molecular basis of PACAP27 binding and VIP receptor activation. The methodology of the NanoBiT tethering may help to provide structural information of unstable complexes. Vasoactive intestinal polypeptide receptor (VIP1R) is a widely expressed class B G protein-coupled receptor and a drug target for the treatment of inflammatory diseases. Here authors report a cryoelectron microscopy structure of human VIP1R bound to PACAP27 and Gs heterotrimer, which provides insights into PACAP27 binding and VIP receptor activation.
WOS关键词VASOACTIVE-INTESTINAL-PEPTIDE ; 3RD INTRACELLULAR LOOP ; VPAC(1) RECEPTOR ; GLP-1 RECEPTOR ; EXPRESSION ; LOCALIZATION ; VALIDATION ; MUTATIONS ; RESIDUES ; BINDING
资助项目National Natural Science Foundation of China[31770796] ; National Natural Science Foundation of China[81922071] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program[2018ZX09711002] ; Shanghai Municipal Science and Technology Major Project[2019SHZDZX02] ; CAS Strategic Priority Research Program[XDB37030103] ; Ministry of Science and Technology (China)[2018YFA0507002] ; National Key Basic Research Program of China[2019YFA0508800] ; Zhejiang Province Science Fund for Distinguished Young Scholars[LR19H310001] ; Fundamental Research Funds for the Central Universities[2019XZZX001-01-06] ; Shanghai Sailing Program[19YF1457600] ; K.C. Wong Education Foundation ; Van Andel Research Institute
WOS研究方向Science & Technology - Other Topics
语种英语
出版者NATURE PUBLISHING GROUP
WOS记录号WOS:000563565300012
源URL[http://119.78.100.183/handle/2S10ELR8/292437]  
专题中国科学院上海药物研究所
通讯作者Zhang, Yan; Xu, H. Eric; Jiang, Yi
作者单位1.Zhejiang Univ, Dept Biophys, Sch Med, Hangzhou 310058, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, 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.Zhejiang Univ, Sir Run Run Shaw Hosp, Dept Pathol, Sch Med, Hangzhou 310058, Peoples R China
6.Van Andel Inst, Ctr Canc & Cell Biol, Program Struct Biol, Grand Rapids, MI USA
推荐引用方式
GB/T 7714		 Duan, Jia,Shen, Dan-dan,Zhou, X. Edward,et al. Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy[J]. NATURE COMMUNICATIONS,2020,11(1):10.
APA Duan, Jia.,Shen, Dan-dan.,Zhou, X. Edward.,Bi, Peng.,Liu, Qiu-feng.,...&Jiang, Yi.(2020).Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy.NATURE COMMUNICATIONS,11(1),10.
MLA Duan, Jia,et al."Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy".NATURE COMMUNICATIONS 11.1(2020):10.

入库方式： OAI收割

来源：上海药物研究所

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