G蛋白偶联受体异源二聚体及其偏向性配体:未来药物研发的新主角

被引：6

作者：

刘路路 ^{[1
,2
]}

陈京 ^{[1
]}

白波 ^{[1
]}

机构：

[1] 济宁医学院神经生物学研究所

[2] 曲阜师范大学

来源：

中国药理学通报 | 2013年 / 29卷 / 10期

关键词：

G蛋白偶联受体; 同源/异源二聚体; 偏向性配体; 病理生理学; 药理学; 共振能量转移;

D O I：

暂无

中图分类号：

R96 [药理学];

学科分类号：

100706 [药理学];

摘要：

不同类型G蛋白偶联受体(GPCRs)之间的异源二聚化作用已得到普遍认可,异源二聚体具有不同于单体和同源二聚体的高阶结构特点,这在一定层次上类似于变构调节机制,使得GPCRs异源二聚体呈现更高的信号特异性和多样性。成功筛选GPCRs异源二聚体的特异配体或偏向性配体,能够为研发降低副作用的药物提供新的策略。该文就GPCRs异源二聚体的信号特点及其偏向性配体的生理药理学价值和筛选GPCRs异源二聚体偏向性配体的技术做一简要综述。

引用

页码：1468 / 1472

页数：5

共 10 条

[1]

Molecular Mechanism of β-Arrestin-Biased Agonism at Seven-Transmembrane Receptors.[J].Eric Reiter;Seungkirl Ahn;Arun K. Shukla;Robert J. Lefkowitz.Annual Review of Pharmacology and Toxicology.2012, 1

[2]

Heterodimerization of human apelin and kappa opioid receptors: Roles in signal transduction.[J].Yalin Li;Jing Chen;Bo Bai;Hui Du;Youwang Liu;Haiqing Liu.Cellular Signalling.2011, 5

[3]

Uncovering GPCR heteromer-biased ligands.[J].Sanam Mustafa;Mohammed Akli Ayoub;Kevin D.G. Pfleger.Drug Discovery Today: Technologies.2010, 1

[4]

Alternative G protein coupling and biased agonism: New insights into melanocortin-4 receptor signalling.[J].Andreas Breit;Thomas R.H. Büch;Ingrid Boekhoff;Hans Jürgen Solinski;Ellen Damm;Thomas Gudermann.Molecular and Cellular Endocrinology.2010, 2

[5]

The impact of GPCR structures on pharmacology and structure-based drug design [J].

Congreve, Miles ;

Marshall, Fiona .

BRITISH JOURNAL OF PHARMACOLOGY, 2010, 159 (05) :986-996

[6]

Recent advances in bioluminescence resonance energy transfer technologies to study GPCR heteromerization.[J].Mohammed A Ayoub;Kevin DG Pfleger.Current Opinion in Pharmacology.2009, 1

[7]

Receptor heteromerization and drug discovery.[J].Raphael Rozenfeld;Lakshmi A. Devi.Trends in Pharmacological Sciences.2009, 3

[8]

β-arrestin-biased ligands at seven-transmembrane receptors [J].

Violin, Jonathan D. ;

Lefkowitz, Robert J. .

TRENDS IN PHARMACOLOGICAL SCIENCES, 2007, 28 (08) :416-422

[9]

Heterodimers of G protein-coupled receptors as novel and distinct drug targets.[J].Raphael Rozenfeld;Fabien M. Décaillot;Adriaan P. IJzerman;Lakshmi A. Devi.Drug Discovery Today: Therapeutic Strategies.2006, 4

[10]

Heterodimerization of β1- and β2-adrenergic receptor subtypes optimizes β-adrenergic modulation of cardiac contractility [J].

Zhu, WZ ;

Chakir, K ;

Zhang, SJ ;

Yang, DM ;

Lavoie, C ;

Bouvier, M ;

Hébert, TE ;

Lakatta, EG ;

Cheng, HP ;

Xiao, RP .

CIRCULATION RESEARCH, 2005, 97 (03) :244-251

← 1 →