G-protein-coupled receptor-signaling components in membrane raft and caveolae microdomains. Handb Exp Pharmacol 2008;167-184.Patel HH, Murray F, and Insel PA. G-protein-coupled receptor-signaling components in membrane raft and caveolae microdomains. Handb Exp Pharmacol: 167-184, 2008....
3.Kobilka, B. The structural basis of G-protein-coupled receptor signaling (Nobel Lecture).Angewandte Chemie52, 6380-6388, doi:10.1002/anie.201302116 (2013). 4.Congreve, M., de Graaf, C., Swain, N. A. & Tate, C. G. Impact of GPCR Structures on Drug Discovery.Cell181, 81-91, d...
G protein-coupled receptors (GPCRs) constitute a large family of receptors that activate intracellular signaling pathways upon detecting specific extracellular ligands. While many aspects of GPCR signaling have been uncovered through decades of studies, some fundamental properties, like its channel capacity...
神经系统中的代谢神经调控通常由G蛋白偶联受体(G Protein-coupled receptors,GPCRs)通过激活异三聚体G蛋白转导信号实现[2]。G蛋白信号调节蛋白(regulator of g protein signaling protein,RGS)可促进其G蛋白信号失活[3]。GPCRs介导除甘氨酸和牛磺酸以外的所有主要神经递质的作用。然而,许多GPCR仍然没有确定的内源性配...
The targeting and modulation of G-protein-coupled receptors (GPCRs) has immense therapeutic potential. A study inNaturenow reports on the successful targeting of intracellular allosteric sites that effectively bias GPCR signaling, which has opened new opportunities to develop safer therapeutic agents. ...
the surface of the receptor, dissociating into its α- and β/γ subunits. Both subunits will then activate their specific effectors, causing the release of second messengers. These messengers are recognised by protein kinases leading to their activation and triggering the signaling cascade towards a...
G 蛋白偶联受体 (G-protein-coupled receptors, GPCRs) 是人类基因组中最大的蛋白质超家族。GPCRs 是一大类七次跨膜的受体蛋白，通过与 G 蛋白偶联，随后调节多种细胞内信号级联反应，以响应激素、神经递质、离子、光、气味、趋化因子和其他刺激 ，参与了众多生理过程包括感光、嗅觉、行为和情绪的调节、自主神经...
信号转导(Signalling transduction):当细胞膜上的受体感受外界信号刺激后,将胞外信号通过跨膜结构转化为胞内信号,并通过胞内信使系统级联放大信号以及蛋白质的可逆磷酸化,调节相应酶或基因的表达,最终引起相应的生理反应,达到维持体内平衡的目的。 G蛋白偶联受体(G-protein-coupled receptor, GPCR):是迄今为止发现的最...
Dysregulation of G-protein-coupled receptor (GPCR) function has been shown to be associated with a growing number of human diseases. In some diseases, mutation of an endogenous GPCR causes the receptor to lose the ability to bind agonist or signal (`loss of function' mutation), whereas another...
GPCR(G Protein-Coupled Receptor),即G蛋白偶联受体,是一大类膜蛋白受体的统称。GPCR是人类基因组编码的最大蛋白家族,广泛分布于中枢神经系统、免疫系统、心血管及视网膜等器官和组织,参与机体发育以及多种生理功能的调控。 GPCR的主体由7段跨细胞质膜的α螺旋结构构成,将信号由胞外转导到胞内(图1)。基于进化同源性...