Structural Basis for Apelin Control of the Human Apelin Receptor

doi:10.1016/j.str.2017.04.008

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	Structural Basis for Apelin Control of the Human Apelin Receptor
	Ma, Yingli 1; Yue, Yang2 ; Ma, Yanbin 1; Zhang, Qing 1; Zhou, Qingtong2 ; Song, Yunpeng 1; Shen, Yuqing 1; Li, Xun 1; Ma, Xiaochuan 1; Li, Chao2,3,4,5 ; Hanson, Michael A.6; Han, Gye Won 7; Sickmier, E. Allen 8; Swaminath, Gayathri 9; Zhao, Suwen2,3 ; Stevens, Raymond C.2,3 ; Hu, Liaoyuan A.1; Zhong, Wenge 1; Zhang, Mingqiang 1; Xu, Fei2,3
	2017-06-06
发表期刊	STRUCTURE (IF:4.4[JCR-2023],4.3[5-Year])
ISSN	0969-2126
卷号	25 期号:6 页码:858-+
发表状态	已发表
DOI	10.1016/j.str.2017.04.008
摘要	Apelin receptor (APJR) is a key regulator of human cardiovascular function and is activated by two different endogenous peptide ligands, apelin and Elabela, each with different isoforms diversified by length and amino acid sequence. Here we report the 2.6-A resolution crystal structure of human APJR in complex with a designed 17-amino-acid apelin mimetic peptide agonist. The structure reveals that the peptide agonist adopts a lactam constrained curved two-site ligand binding mode. Combined with mutation analysis and molecular dynamics simulations with apelin-13 binding to the wild-type APJR, this structure provides a mechanistic understanding of apelin recognition and binding specificity. Comparison of this structure with that of other peptide receptors suggests that endogenous peptide ligands with a high degree of conformational flexibility may bind and modulate the receptors via a similar two site binding mechanism.
收录类别	SCI
语种	英语
资助项目	Natural Science Foundation of Shanghai grant[16ZR1448500]
WOS研究方向	Biochemistry & Molecular Biology ; Biophysics ; Cell Biology
WOS类目	Biochemistry & Molecular Biology ; Biophysics ; Cell Biology
WOS记录号	WOS:000405599500007
出版者	CELL PRESS
WOS关键词	PROTEIN-COUPLED RECEPTORS ; KAPPA-OPIOID RECEPTOR ; IMMUNODEFICIENCY-VIRUS TYPE-1 ; A(2A) ADENOSINE RECEPTOR ; CRYSTALLIZING MEMBRANE ; ANGIOTENSIN RECEPTOR ; LIPIDIC MESOPHASES ; HEART-FAILURE ; AMINO-ACIDS ; APJ
原始文献类型	Article
通讯作者	Xu, Fei
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/2915
专题	iHuman研究所生命科学与技术学院 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_PI研究组_徐菲组 iHuman研究所_PI研究组_赵素文组生命科学与技术学院_硕士生
通讯作者	Xu, Fei
作者单位	1.Amgen Biopharmaceut R&D Shanghai Co Ltd, Amgen Asia R&D Ctr, Shanghai 201210, Peoples R China 2.ShanghaiTech Univ, iHuman Inst, 2F Bldg 6,99 Haike Rd, Shanghai 201210, Peoples R China 3.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China 5.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 6.GPCR Consortium, San Marcos, CA 92078 USA 7.Univ Southern Calif, Dept Chem, Bridge Inst, Los Angeles, CA 90089 USA 8.Amgen Inc, Dept Mol Engn, Therapeut Discovery, 360 BinneySt, Cambridge, MA 02142 USA 9.Amgen Inc, Cardiovasc Disorders, 1120 Vet Blvd, San Francisco, CA 94080 USA
通讯作者单位	iHuman研究所; 生命科学与技术学院
推荐引用方式 GB/T 7714	Ma, Yingli,Yue, Yang,Ma, Yanbin,et al. Structural Basis for Apelin Control of the Human Apelin Receptor[J]. STRUCTURE,2017,25(6):858-+.
APA	Ma, Yingli.,Yue, Yang.,Ma, Yanbin.,Zhang, Qing.,Zhou, Qingtong.,...&Xu, Fei.(2017).Structural Basis for Apelin Control of the Human Apelin Receptor.STRUCTURE,25(6),858-+.
MLA	Ma, Yingli,et al."Structural Basis for Apelin Control of the Human Apelin Receptor".STRUCTURE 25.6(2017):858-+.