Structure and Function of Peptide-Binding G Protein-Coupled Receptors

doi:10.1016/j.jmb.2017.06.022

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	Structure and Function of Peptide-Binding G Protein-Coupled Receptors
	Wu, Fan1 ; Song, Gaojie1 ; de Graaf, Chris 2; Stevens, Raymond C.1
	2017-08-18
发表期刊	JOURNAL OF MOLECULAR BIOLOGY (IF:4.7[JCR-2023],4.9[5-Year])
ISSN	0022-2836
卷号	429 期号:17 页码:2726-2745
发表状态	已发表
DOI	10.1016/j.jmb.2017.06.022
摘要	G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors and are important human drug targets. Of the 826 human GPCRs, 118 of them recognize endogenous peptide or protein ligands, and 30 of the 118 are targeted by approved drug molecules, including the very high-profile class B glucagon-like peptide 1 receptor. In this review, we analyze the 21 experimentally determined three-dimensional structures of the known peptide-binding GPCRs in relation to the endogenous peptides and drug molecules that modulate their cell signaling processes. Our integrated analyses reveal that half of the marketed drugs and most of the drugs in clinical trials that interact with peptide GPCRs are small molecules with a wide range of binding modes distinct from those of large peptide ligands. As we continue to collect additional data on these receptors from orthogonal approaches, including nuclear magnetic resonance and electron microscopy, we are beginning to understand how these receptors interact with their ligands at the molecular level and how improving the pharmacology of GPCR signal transduction requires us to study these receptors using multiple biophysical techniques. (C) 2017 Elsevier Ltd. All rights reserved.
收录类别	SCI
语种	英语
资助项目	European Cooperation in Science and Technology Action[CM1207 GLISTEN]
WOS研究方向	Biochemistry & Molecular Biology
WOS类目	Biochemistry & Molecular Biology
WOS记录号	WOS:000408179100013
出版者	ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD
WOS关键词	CORTICOTROPIN-RELEASING-FACTOR ; CLASS-B GPCR ; NOCICEPTIN/ORPHANIN FQ RECEPTOR ; RESOLUTION CRYSTAL-STRUCTURE ; GLUCAGON-LIKE PEPTIDE-1 ; KAPPA-OPIOID RECEPTOR ; CRYO-EM STRUCTURE ; INTERNATIONAL-UNION ; CHEMOKINE RECEPTOR ; SMALL-MOLECULE
原始文献类型	Review
通讯作者	Stevens, Raymond C.
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/9874
专题	iHuman研究所生命科学与技术学院 iHuman研究所_特聘教授组_Raymond Stevens组 iHuman研究所_PI研究组_刘志杰组生命科学与技术学院_博士生
通讯作者	Stevens, Raymond C.
作者单位	1.ShanghaiTech Univ, iHuman Inst, 393 Middle Huaxia Rd, Shanghai 201210, Peoples R China 2.Vrije Univ Amsterdam, AIMMS, Fac Sci, Div Med Chem, De Boelelaan 1108, NL-1081 HZ Amsterdam, Netherlands
第一作者单位	iHuman研究所
通讯作者单位	iHuman研究所
第一作者的第一单位	iHuman研究所
推荐引用方式 GB/T 7714	Wu, Fan,Song, Gaojie,de Graaf, Chris,et al. Structure and Function of Peptide-Binding G Protein-Coupled Receptors[J]. JOURNAL OF MOLECULAR BIOLOGY,2017,429(17):2726-2745.
APA	Wu, Fan,Song, Gaojie,de Graaf, Chris,&Stevens, Raymond C..(2017).Structure and Function of Peptide-Binding G Protein-Coupled Receptors.JOURNAL OF MOLECULAR BIOLOGY,429(17),2726-2745.
MLA	Wu, Fan,et al."Structure and Function of Peptide-Binding G Protein-Coupled Receptors".JOURNAL OF MOLECULAR BIOLOGY 429.17(2017):2726-2745.