The importance of ligands for G protein-coupled receptor stability

doi:10.1016/j.tibs.2014.12.005

KMS > iHuman研究所 > 特聘教授组 > Raymond Stevens组

	The importance of ligands for G protein-coupled receptor stability
	Zhang, Xianjun; Stevens, Raymond C.; Xu, Fei
	2015-02
发表期刊	TRENDS IN BIOCHEMICAL SCIENCES (IF:11.6[JCR-2023],12.5[5-Year])
ISSN	0968-0004
卷号	40 期号:2 页码:79-87
发表状态	已发表
DOI	10.1016/j.tibs.2014.12.005
摘要	Traditionally, G protein-coupled receptor (GPCR) activity has been characterized by ligand properties including affinity (K-i), potency (IC50/EC50), efficacy (E-max), and kinetics (K-on/K-off). These properties are related to ligand residence time, a general index of drug-target interaction in vivo. Recent GPCR structure-function breakthroughs have all required ligand stabilization of the receptor in some manner, highlighting the natural instability of these important cell surface receptors. This research has initiated a new era of discovery that highlights the importance of ligand-receptor interactions beyond the traditional mindset. We propose that receptor stability is related to receptor folding and residence in the cell membrane, affording a new dimension that should be considered when studying receptor function.
关键词	GPCR stabilization ligand residence time receptor residence time
收录类别	SCI
语种	英语
WOS研究方向	Biochemistry & Molecular Biology
WOS类目	Biochemistry & Molecular Biology
WOS记录号	WOS:000349586700003
出版者	ELSEVIER SCIENCE LONDON
WOS关键词	MUSCARINIC ACETYLCHOLINE-RECEPTOR ; RESOLUTION CRYSTAL-STRUCTURE ; ADENOSINE A(2A) RECEPTOR ; HUMAN P2Y(12) RECEPTOR ; STRUCTURAL BASIS ; OPIOID RECEPTOR ; SEROTONIN RECEPTORS ; MEMBRANE-PROTEINS ; COMPLEX ; GPCR
原始文献类型	Review
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/2263
专题	iHuman研究所_特聘教授组_Raymond Stevens组生命科学与技术学院 iHuman研究所 iHuman研究所_PI研究组_徐菲组生命科学与技术学院_博士生
通讯作者	Xu, Fei
作者单位	ShanghaiTech Univ, iHuman Inst, Shanghai 201210, Peoples R China
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	Zhang, Xianjun,Stevens, Raymond C.,Xu, Fei. The importance of ligands for G protein-coupled receptor stability[J]. TRENDS IN BIOCHEMICAL SCIENCES,2015,40(2):79-87.
APA	Zhang, Xianjun,Stevens, Raymond C.,&Xu, Fei.(2015).The importance of ligands for G protein-coupled receptor stability.TRENDS IN BIOCHEMICAL SCIENCES,40(2),79-87.
MLA	Zhang, Xianjun,et al."The importance of ligands for G protein-coupled receptor stability".TRENDS IN BIOCHEMICAL SCIENCES 40.2(2015):79-87.