G蛋白结合受体的分子特征
A J Venkatakrishnan1, Xavier Deupi, Guillaume Lebon
1MRC Laboratory of Molecular Biology, Hills Road, Cambridge CB2 0QH, UK. ajv@mrc-lmb.cam.ac.uk
Nature
|February 15, 2013
概括
G蛋白结合受体 (GPCR) 是一种重要的膜蛋白. 新的研究揭示了GPCR中保存的结构网络,为药物开发提供了对联体结合和激活的见解.
科学领域:
- 生物化学和结构生物学.
- 分子和系统生物学分子和系统生物学
背景情况:
- G蛋白结合受体 (GPCR) 是关键的膜蛋白,参与细胞信号传递.
- 它们是众多治疗药物的目标,突出了它们在医学上的重要性.
- 最近的进展为医学上重要的GPCRs提供了新的结构和功能洞察力.
研究的目的:
- 系统地分析高分辨率的GPCR结构.
- 识别保存的结构特征,了解带结合和激活机制.
- 为新的治疗策略整合分子和系统生物学.
主要方法:
- 高分辨率G蛋白结合受体 (GPCR) 结构的系统分析.
- 对GPCR结构进行比较分析,以确定保存的非共价接触.
- 在受体激活过程中检查连接体结合和形状变化.
主要成果:
- 发现了定义G蛋白结合受体 (GPCR) 折叠的非共价接触的保存网络.
- 鉴定出了连接因子结合的特征特征.
- 阐明了受体激活过程中的关键形状变化.
结论:
- 一个保存的结构网络支着G蛋白结合受体 (GPCR) 折叠.
- 了解GPCRs的分子和系统生物学对于开发新疗法至关重要.
- 这项研究为针对GPCR的个性化医学方法铺平了道路.
相关概念视频
G Protein-coupled Receptors
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G-protein Coupled Receptors
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
Transducer Mechanism: G Protein–Coupled Receptors
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
GPCRs are also called heptahelical, 7TM, or...
Assembly of Signaling Complexes
Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...


