Molecular signatures of G-protein-coupled receptors

被引：1235

作者：

Venkatakrishnan, A. J. ^{[1
]}

Deupi, Xavier ^{[2
]}

Lebon, Guillaume ^{[1
,3
,4
,5
,6
]}

Tate, Christopher G. ^{[1
]}

Schertler, Gebhard F. ^{[2
,7
]}

Babu, M. Madan ^{[1
]}

机构：

[1] MRC, Mol Biol Lab, Cambridge CB2 0QH, England

[2] Paul Scherrer Inst, CH-5232 Villigen, Switzerland

[3] CNRS, UMR 5203, Inst Genom Fonct, F-34094 Montpellier, France

[4] CNRS, INSERM, U661, F-34094 Montpellier, France

[5] Univ Montpellier I, UMR 5203, F-34094 Montpellier, France

[6] Univ Montpellier 2, UMR 5203, F-34094 Montpellier, France

[7] ETH, Dept Biol, CH-8093 Zurich, Switzerland

来源：

NATURE | 2013年 / 494卷 / 7436期

基金：

瑞士国家科学基金会; 英国医学研究理事会;

关键词：

RESOLUTION CRYSTAL-STRUCTURE; ADENOSINE A(2A) RECEPTOR; BETA(2)-ADRENERGIC RECEPTOR; STRUCTURAL INSIGHTS; ALLOSTERIC COMMUNICATION; DISTINCT CONFORMATIONS; TRANSMEMBRANE HELICES; ACTIVATED STATE; COMPLEX; AGONIST;

D O I：

10.1038/nature11896

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

070301 [无机化学]; 070403 [天体物理学]; 070507 [自然资源与国土空间规划学]; 090105 [作物生产系统与生态工程];

摘要：

G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that sense signalling molecules such as hormones and neurotransmitters, and are the targets of several prescribed drugs. Recent exciting developments are providing unprecedented insights into the structure and function of several medically important GPCRs. Here, through a systematic analysis of high-resolution GPCR structures, we uncover a conserved network of non-covalent contacts that defines the GPCR fold. Furthermore, our comparative analysis reveals characteristic features of ligand binding and conformational changes during receptor activation. A holistic understanding that integrates molecular and systems biology of GPCRs holds promise for new therapeutics and personalized medicine.

引用

页码：185 / 194

页数：10

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