From the Life Sciences Institute and.
From the Life Sciences Institute and; Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48109-2216.
J Biol Chem. 2011 Mar 11;286(10):7715-7721. doi: 10.1074/jbc.R109.051847. Epub 2011 Jan 3.
G protein-coupled receptors (GPCRs) represent the largest class of integral membrane protein receptors in the human genome. Despite the great diversity of ligands that activate these GPCRs, they interact with a relatively small number of intracellular proteins to induce profound physiological change. Both heterotrimeric G proteins and GPCR kinases are well known for their ability to specifically recognize GPCRs in their active state. Recent structural studies now suggest that heterotrimeric G proteins and GPCR kinases identify activated receptors via a common molecular mechanism despite having completely different folds.
G 蛋白偶联受体(GPCRs)是人类基因组中最大的一类整合膜蛋白受体。尽管激活这些 GPCR 的配体种类繁多,但它们与相对较少的细胞内蛋白相互作用,从而引发深刻的生理变化。异三聚体 G 蛋白和 GPCR 激酶以其识别处于激活状态的 GPCR 的能力而闻名。最近的结构研究表明,尽管异三聚体 G 蛋白和 GPCR 激酶的结构完全不同,但它们通过共同的分子机制识别激活的受体。