Structural basis of peptide recognition and activation of endothelin receptors

doi:10.1038/s41467-023-36998-9

	Structural basis of peptide recognition and activation of endothelin receptors
	Ji, Yujie 1,2; Duan, Jia 1,2,3; Yuan, Qingning 1; He, Xinheng 1,2; Yang, Gong 4; Zhu, Shengnan 5; Wu, Kai 1; Hu, Wen 1; Gao, Tianyu6 ; Cheng, Xi 1,2; Jiang, Hualiang1,2,6,7 ; Xu, H. Eric1,2,6 ; Jiang, Yi6,7
	2023-12-01
发表期刊	NATURE COMMUNICATIONS; (IF:14.7[JCR-2023],16.1[5-Year])
ISSN	2041-1723
EISSN	2041-1723
卷号	14 期号:1
发表状态	已发表
DOI	10.1038/s41467-023-36998-9
摘要	Endothelin system comprises three endogenous 21-amino-acid peptide ligands endothelin-1, -2, and -3 (ET-1/2/3), and two G protein-coupled receptor (GPCR) subtypes—endothelin receptor A (ETAR) and B (ETBR). Since ET-1, the first endothelin, was identified in 1988 as one of the most potent endothelial cell-derived vasoconstrictor peptides with long-lasting actions, the endothelin system has attracted extensive attention due to its critical role in vasoregulation and close relevance in cardiovascular-related diseases. Here we present three cryo-electron microscopy structures of ETAR and ETBR bound to ET-1 and ETBR bound to the selective peptide IRL1620. These structures reveal a highly conserved recognition mode of ET-1 and characterize the ligand selectivity by ETRs. They also present several conformation features of the active ETRs, thus revealing a specific activation mechanism. Together, these findings deepen our understanding of endothelin system regulation and offer an opportunity to design selective drugs targeting specific ETR subtypes.
学科门类	Chemistry (all) ; Biochemistry, Genetics and Molecular Biology (all) ; Multidisciplinary ; Physics and Astronomy (all)
URL	查看原文
收录类别	SCOPUS ; SCI
语种	英语
资助项目	null[32171187] ; null[82121005] ; null[32130022] ; null[2018YFA0507002] ; null[2019SHZDZX02] ; null[XDB37030103]
WOS研究方向	Science & Technology - Other Topics
WOS类目	Multidisciplinary Sciences
WOS记录号	WOS:000957599200017
出版者	NATURE PORTFOLIO
原始文献类型	Article
Scopus 记录号	2-s2.0-85149501614
来源库	SCOPUS
引用统计	正在获取...
文献类型	期刊论文
条目标识符	https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/286504
专题	生命科学与技术学院_硕士生生命科学与技术学院免疫化学研究所_特聘教授组_蒋华良组生命科学与技术学院_特聘教授组_徐华强组生命科学与技术学院_博士生
通讯作者	Duan, Jia; Xu, H. Eric; Jiang, Yi
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Zhongshan Inst Drug Discovery, Zhongshan, Peoples R China 4.Xiamen Univ, Sch Life Sci, State Key Lab Cellular Stress Biol, Xiamen 361005, Fujian, Peoples R China 5.Macau Univ Sci & Technol, Sch Pharm, Macau 999078, Peoples R China 6.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 7.Lingang Lab, Shanghai 200031, Peoples R China
通讯作者单位	生命科学与技术学院
推荐引用方式 GB/T 7714	Ji, Yujie,Duan, Jia,Yuan, Qingning,et al. Structural basis of peptide recognition and activation of endothelin receptors[J]. NATURE COMMUNICATIONS;,2023,14(1).
APA	Ji, Yujie.,Duan, Jia.,Yuan, Qingning.,He, Xinheng.,Yang, Gong.,...&Jiang, Yi.(2023).Structural basis of peptide recognition and activation of endothelin receptors.NATURE COMMUNICATIONS;,14(1).
MLA	Ji, Yujie,et al."Structural basis of peptide recognition and activation of endothelin receptors".NATURE COMMUNICATIONS; 14.1(2023).