From G Protein-coupled Receptor Structure Resolution to Rational Drug Design

被引：72

作者：

Jazayeri, Ali ^{[1
]}

Dias, Joao M. ^{[1
]}

Marshall, Fiona H. ^{[1
]}

机构：

[1] Heptares Therapeut Ltd, Welwyn Garden City AL7 3AX, Herts, England

来源：

JOURNAL OF BIOLOGICAL CHEMISTRY | 2015年 / 290卷 / 32期

关键词：

ADENOSINE A(2A) RECEPTOR; CRYSTAL-STRUCTURE; DYNAMIC PROCESS; LIGAND-BINDING; DISCOVERY; INSIGHTS; AGONIST; COMPLEX; IDENTIFICATION; ANTAGONISTS;

D O I：

10.1074/jbc.R115.668251

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A number of recent technical solutions have led to significant advances in G protein-coupled receptor (GPCR) structural biology. Apart from a detailed mechanistic view of receptor activation, the new structures have revealed novel ligand binding sites. Together, these insights provide avenues for rational drug design to modulate the activities of these important drug targets. The application of structural data to GPCR drug discovery ushers in an exciting era with the potential to improve existing drugs and discover new ones. In this review, we focus on technical solutions that have accelerated GPCR crystallography as well as some of the salient findings from structures that are relevant to drug discovery. Finally, we outline some of the approaches used in GPCR structure based drug design.

引用

页码：19489 / 19495

页数：7

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