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Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism

文献类型：期刊论文

作者Duan, Jia3,4,5; He, Xin-Heng3,4; Li, Shu-Jie2,4; Xu, H. Eric1,3,4
刊名NATURE REVIEWS ENDOCRINOLOGY
出版日期2024-02-29
页码17
ISSN号1759-5029
DOI10.1038/s41574-024-00957-1
通讯作者Duan, Jia(duanjia@simm.ac.cn) ; Xu, H. Eric(eric.xu@simm.ac.cn)
英文摘要G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors, with many GPCRs having crucial roles in endocrinology and metabolism. Cryogenic electron microscopy (cryo-EM) has revolutionized the field of structural biology, particularly regarding GPCRs, over the past decade. Since the first pair of GPCR structures resolved by cryo-EM were published in 2017, the number of GPCR structures resolved by cryo-EM has surpassed the number resolved by X-ray crystallography by 30%, reaching >650, and the number has doubled every similar to 0.63 years for the past 6 years. At this pace, it is predicted that the structure of 90% of all human GPCRs will be completed within the next 5-7 years. This Review highlights the general structural features and principles that guide GPCR ligand recognition, receptor activation, G protein coupling, arrestin recruitment and regulation by GPCR kinases. The Review also highlights the diversity of GPCR allosteric binding sites and how allosteric ligands could dictate biased signalling that is selective for a G protein pathway or an arrestin pathway. Finally, the authors use the examples of glycoprotein hormone receptors and glucagon-like peptide 1 receptor to illustrate the effect of cryo-EM on understanding GPCR biology in endocrinology and metabolism, as well as on GPCR-related endocrine diseases and drug discovery.
WOS关键词PROTEIN-COUPLED RECEPTOR ; HORMONE SECRETAGOGUE RECEPTOR ; THYROID-STIMULATING HORMONE ; HUMAN THYROTROPIN RECEPTOR ; CALCIUM-SENSING RECEPTOR ; V2 VASOPRESSIN RECEPTOR ; CRYO-EM STRUCTURE ; CRYSTAL-STRUCTURE ; GLP-1 RECEPTOR ; NEPHROGENIC SYNDROME
资助项目CAS Strategic Priority Research Program[XDB37030103] ; Shanghai Municipal Science and Technology Major Project ; National Natural Science Foundation of China[82373881] ; National Key R&D Program of China[2022YFC2703105] ; Young Elite Scientists Sponsorship Program by CAST[2022QNRC001] ; Shanghai Sailing Program[23YF1456800] ; Youth Innovation Promotion Association of Chinese Academy of Sciences
WOS研究方向Endocrinology & Metabolism
语种英语
WOS记录号WOS:001178536200001
出版者NATURE PORTFOLIO
源URL[http://119.78.100.183/handle/2S10ELR8/310157]  
专题新药研究国家重点实验室
通讯作者Duan, Jia; Xu, H. Eric
作者单位1.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai, Peoples R China
2.Fujian Med Univ Union Hosp, Dept Tradit Chinese Med, Fuzhou, Fujian, Peoples R China
3.Univ Chinese Acad Sci, Beijing, Peoples R China
4.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai, Peoples R China
5.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan, Peoples R China
推荐引用方式
GB/T 7714		 Duan, Jia,He, Xin-Heng,Li, Shu-Jie,et al. Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism[J]. NATURE REVIEWS ENDOCRINOLOGY,2024:17.
APA Duan, Jia,He, Xin-Heng,Li, Shu-Jie,&Xu, H. Eric.(2024).Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism.NATURE REVIEWS ENDOCRINOLOGY,17.
MLA Duan, Jia,et al."Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism".NATURE REVIEWS ENDOCRINOLOGY (2024):17.

入库方式： OAI收割

来源：上海药物研究所

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