Molecular biology of adrenergic receptors: model systems for the study of G-protein-mediated signal transduction.

Blood vessels Pub Date : 1991-01-01 DOI:10.1159/000158848
C M Fraser
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引用次数: 9

Abstract

Elucidation of the gene structure of several receptors known to mediate the signal of hormone or transmitter binding to intracellular effector systems through guanine-nucleotide-binding proteins (G proteins) has revealed that these receptors comprise a super-family of related proteins. The hallmark of all G-protein-linked receptors is a presumed topography of 7 membrane-spanning loops, analogous to the structure of bacteriorhodopsin. Members of this gene superfamily contain regions, particularly with the hydrophobic domains, of homologous sequence. The expression of G-protein-linked receptors in heterologous cell systems has allowed for the study of the pharmacological and biochemical properties of individual receptor subtypes in a manner not previously possible with intact tissues containing multiple receptors. Site-directed mutagenesis experiments have identified many conserved amino acids which are involved in ligand binding, receptor activation by agonists and receptor-G protein coupling, and suggest that the conservation of receptor structure throughout this gene family may reflect a conservation of important functional domains within these proteins.

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肾上腺素能受体的分子生物学:研究g蛋白介导的信号转导的模型系统。
通过鸟嘌呤核苷酸结合蛋白(G蛋白)介导激素或递质结合到细胞内效应系统的信号的几个受体的基因结构的阐明表明,这些受体包括一个超家族的相关蛋白。所有g蛋白连接受体的标志是假定的7个跨膜环的地形,类似于细菌视紫红质的结构。该基因超家族的成员包含同源序列的区域,特别是疏水区域。g蛋白连接受体在异源细胞系统中的表达使得研究单个受体亚型的药理学和生化特性成为可能,这是以前不可能在含有多个受体的完整组织中进行的。位点定向诱变实验已经鉴定出许多保守的氨基酸,它们参与配体结合、受体激动剂激活和受体- g蛋白偶联,并表明该基因家族中受体结构的保守可能反映了这些蛋白质中重要功能域的保守。
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