G蛋白偶联受体激活的结构见解
Structural insights into G-protein-coupled receptor activation.
作者信息
Weis William I, Kobilka Brian K
机构信息
Department of Molecular & Cellular Physiology, Stanford University School of Medicine, USA.
出版信息
Curr Opin Struct Biol. 2008 Dec;18(6):734-40. doi: 10.1016/j.sbi.2008.09.010. Epub 2008 Nov 17.
Abstract
G-protein-coupled receptors (GPCRs) are the largest family of eukaryotic plasma membrane receptors, and are responsible for the majority of cellular responses to external signals. GPCRs share a common architecture comprising seven transmembrane (TM) helices. Binding of an activating ligand enables the receptor to catalyze the exchange of GTP for GDP in a heterotrimeric G protein. GPCRs are in a conformational equilibrium between inactive and activating states. Crystallographic and spectroscopic studies of the visual pigment rhodopsin and two beta-adrenergic receptors have defined some of the conformational changes associated with activation.
摘要
G蛋白偶联受体（GPCRs）是真核细胞质膜受体中最大的家族，负责细胞对外部信号的大部分反应。GPCRs具有共同的结构，包括七个跨膜（TM）螺旋。激活配体的结合使受体能够催化异源三聚体G蛋白中GTP与GDP的交换。GPCRs在失活状态和激活状态之间处于构象平衡。对视觉色素视紫红质和两种β-肾上腺素能受体的晶体学和光谱学研究已经确定了一些与激活相关的构象变化。
相似文献
1
Structural insights into G-protein-coupled receptor activation.G蛋白偶联受体激活的结构见解
Curr Opin Struct Biol. 2008 Dec;18(6):734-40. doi: 10.1016/j.sbi.2008.09.010. Epub 2008 Nov 17.
2
Agonist-induced conformational changes in bovine rhodopsin: insight into activation of G-protein-coupled receptors.激动剂诱导的牛视紫红质构象变化：深入了解G蛋白偶联受体的激活
J Mol Biol. 2008 Oct 3;382(2):539-55. doi: 10.1016/j.jmb.2008.06.084. Epub 2008 Jul 7.
3
The Molecular Basis of G Protein-Coupled Receptor Activation.G 蛋白偶联受体激活的分子基础。
Annu Rev Biochem. 2018 Jun 20;87:897-919. doi: 10.1146/annurev-biochem-060614-033910.
4
A G protein-coupled receptor at work: the rhodopsin model.工作中的 G 蛋白偶联受体：视紫红质模型。
Trends Biochem Sci. 2009 Nov;34(11):540-52. doi: 10.1016/j.tibs.2009.07.005. Epub 2009 Oct 21.
5
Activation of G protein-coupled receptors: beyond two-state models and tertiary conformational changes.G蛋白偶联受体的激活：超越双态模型和三级构象变化
Annu Rev Pharmacol Toxicol. 2008;48:107-41. doi: 10.1146/annurev.pharmtox.48.113006.094630.
6
G protein-coupled receptors--recent advances.G蛋白偶联受体——最新进展
Acta Biochim Pol. 2012;59(4):515-29. Epub 2012 Dec 18.
7
Activation of G-protein-coupled receptors: a common molecular mechanism.G蛋白偶联受体的激活：一种常见的分子机制。
Trends Endocrinol Metab. 2003 Nov;14(9):431-7. doi: 10.1016/j.tem.2003.09.007.
8
FoldGPCR: structure prediction protocol for the transmembrane domain of G protein-coupled receptors from class A.FoldGPCR：A 类 G 蛋白偶联受体跨膜结构域的结构预测方案。
Proteins. 2010 Aug 1;78(10):2189-201. doi: 10.1002/prot.22731.
9
Active state-like conformational elements in the beta2-AR and a photoactivated intermediate of rhodopsin identified by dynamic properties of GPCRs.通过GPCR的动态特性鉴定出的β2肾上腺素能受体中的活性状态样构象元件和视紫红质的光激活中间体。
Biochemistry. 2008 Jul 15;47(28):7317-21. doi: 10.1021/bi800442g. Epub 2008 Jun 18.
10
Comparison of class A and D G protein-coupled receptors: common features in structure and activation.A类和D类G蛋白偶联受体的比较：结构与激活的共同特征
Biochemistry. 2005 Jun 28;44(25):8959-75. doi: 10.1021/bi047316u.
引用本文的文献
1
EnGCI: enhancing GPCR-compound interaction prediction via large molecular models and KAN network.EnGCI：通过大分子模型和KAN网络增强GPCR-化合物相互作用预测
BMC Biol. 2025 May 15;23(1):136. doi: 10.1186/s12915-025-02238-3.
2
Orphan G protein-coupled receptors: the ongoing search for a home.孤儿G蛋白偶联受体：仍在寻找归属
Front Pharmacol. 2024 Feb 29;15:1349097. doi: 10.3389/fphar.2024.1349097. eCollection 2024.
3
Fully activated structure of the sterol-bound Smoothened GPCR-Gi protein complex.固醇结合的 Smoothened GPCR-Gi 蛋白复合物的完全激活结构。
Proc Natl Acad Sci U S A. 2023 Dec 5;120(49):e2300919120. doi: 10.1073/pnas.2300919120. Epub 2023 Nov 28.
4
In Silico Approaches to Identify Polyphenol Compounds as α-Glucosidase and α-Amylase Inhibitors against Type-II Diabetes.计算机辅助方法鉴定多酚类化合物作为 II 型糖尿病的α-葡萄糖苷酶和α-淀粉酶抑制剂
Biomolecules. 2021 Dec 14;11(12):1877. doi: 10.3390/biom11121877.
5
Mapping Angiotensin II Type 1 Receptor-Biased Signaling Using Proximity Labeling and Proteomics Identifies Diverse Actions of Biased Agonists.应用邻近标记和蛋白质组学绘制血管紧张素 II 型 1 受体偏向性信号转导图谱，鉴定出多种偏向激动剂的作用。
J Proteome Res. 2021 Jun 4;20(6):3256-3267. doi: 10.1021/acs.jproteome.1c00080. Epub 2021 May 5.
6
The mutational landscape of human olfactory G protein-coupled receptors.人类嗅觉 G 蛋白偶联受体的突变景观。
BMC Biol. 2021 Feb 5;19(1):21. doi: 10.1186/s12915-021-00962-0.
7
Structural Transition States Explored With Minimalist Coarse Grained Models: Applications to Calmodulin.用极简粗粒度模型探索结构过渡态：应用于钙调蛋白
Front Mol Biosci. 2019 Oct 15;6:104. doi: 10.3389/fmolb.2019.00104. eCollection 2019.
8
Molecular docking, molecular modeling, and molecular dynamics studies of azaisoflavone as dual COX-2 inhibitors and TP receptor antagonists.氮杂异黄酮作为双重COX-2抑制剂和TP受体拮抗剂的分子对接、分子建模及分子动力学研究
J Mol Model. 2018 Feb 26;24(3):69. doi: 10.1007/s00894-018-3620-0.
9
Evolution of nonspectral rhodopsin function at high altitudes.高海拔环境中非光谱视紫红质功能的进化。
Proc Natl Acad Sci U S A. 2017 Jul 11;114(28):7385-7390. doi: 10.1073/pnas.1705765114. Epub 2017 Jun 22.
10
Protein Regulation in Signal Transduction.信号转导中的蛋白质调控
Cold Spring Harb Perspect Biol. 2016 Jun 1;8(6):a005918. doi: 10.1101/cshperspect.a005918.
本文引用的文献
1
Structure of a beta1-adrenergic G-protein-coupled receptor.β1-肾上腺素能G蛋白偶联受体的结构
Nature. 2008 Jul 24;454(7203):486-91. doi: 10.1038/nature07101. Epub 2008 Jun 25.
2
Crystal structure of the ligand-free G-protein-coupled receptor opsin.无配体G蛋白偶联受体视蛋白的晶体结构。
Nature. 2008 Jul 10;454(7201):183-7. doi: 10.1038/nature07063. Epub 2008 Jun 18.
3
A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor.人β2-肾上腺素能受体2.8埃的结构确定了一个特定的胆固醇结合位点。
Structure. 2008 Jun;16(6):897-905. doi: 10.1016/j.str.2008.05.001.
4
High-resolution distance mapping in rhodopsin reveals the pattern of helix movement due to activation.视紫红质中的高分辨率距离映射揭示了激活引起的螺旋运动模式。
Proc Natl Acad Sci U S A. 2008 May 27;105(21):7439-44. doi: 10.1073/pnas.0802515105. Epub 2008 May 19.
5
Crystal structure of squid rhodopsin.鱿鱼视紫红质的晶体结构。
Nature. 2008 May 15;453(7193):363-7. doi: 10.1038/nature06925.
6
Crystal structure of squid rhodopsin with intracellularly extended cytoplasmic region.具有细胞内延伸细胞质区域的鱿鱼视紫红质的晶体结构。
J Biol Chem. 2008 Jun 27;283(26):17753-6. doi: 10.1074/jbc.C800040200. Epub 2008 May 6.
7
Conformational thermostabilization of the beta1-adrenergic receptor in a detergent-resistant form.β1肾上腺素能受体以耐去污剂形式存在时的构象热稳定性
Proc Natl Acad Sci U S A. 2008 Jan 22;105(3):877-82. doi: 10.1073/pnas.0711253105. Epub 2008 Jan 11.
8
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor.一种工程化人β2-肾上腺素能G蛋白偶联受体的高分辨率晶体结构
Science. 2007 Nov 23;318(5854):1258-65. doi: 10.1126/science.1150577. Epub 2007 Oct 25.
9
GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function.G蛋白偶联受体工程为β2肾上腺素能受体功能带来了高分辨率的结构见解。
Science. 2007 Nov 23;318(5854):1266-73. doi: 10.1126/science.1150609. Epub 2007 Oct 25.
10
A monoclonal antibody for G protein-coupled receptor crystallography.用于G蛋白偶联受体晶体学的单克隆抗体。
Nat Methods. 2007 Nov;4(11):927-9. doi: 10.1038/nmeth1112. Epub 2007 Oct 21.
Zotero 插件