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A tale of two sites: How ubiquitination of a G protein-coupled receptor is coupled to its lysosomal trafficking from distinct receptor domains

机译:关于两个位点的故事:G蛋白偶联受体的泛素化如何与其来自不同受体域的溶酶体运输相偶联

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摘要

The β2-adrenergic receptor (β2AR) is a prototypical Gs-coupled receptor belonging to the superfamily of seven transmembrane spanning heptahelical receptors (7TMRs or G protein-coupled receptors [GPCRs])—therapeutically the most diverse and accessible class of cell surface receptors. The classic pathway of β2AR signaling (Fig. 1) is triggered by activation of the heterotrimeric G protein Gs by agonists (catecholamines—noradrenaline and adrenaline). This in turn activates adenylyl cyclase leading to the generation of second messenger signaling molecules (cyclic adenosine monophosphates, cAMP) which subsequently activate protein kinase A (PKA) as well as some ion channels, such as the class C type of L-type calcium channels, Cav1.2.31 Here in we review how trafficking and signaling of the β2AR is regulated by the post-translational modification, ubiquitination.1
机译:β2-肾上腺素能受体(β2AR)是一种典型的Gs偶联受体,属于七个跨膜跨七螺旋受体(7TMRs或G蛋白偶联受体[GPCR])的超家族,这是细胞表面受体中最多样化和可访问的一类。 β2AR信号传导的经典途径(图1)由激动剂(儿茶酚胺-去甲肾上腺素和肾上腺素)激活异三聚体G蛋白Gs触发。这继而激活腺苷酸环化酶,导致生成第二信使信号分子(环状腺苷单磷酸,cAMP),随后激活蛋白激酶A(PKA)以及一些离子通道,例如C类L型钙通道,Cav1.2.31在这里,我们综述了翻译后修饰泛素化如何调控β2AR的运输和信号传导。

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