G蛋白偶联受体与G蛋白相互作用的最新研究进展

Advances in the research of interaction between G protein-coupled receptors and G proteins

传统观念认为,在激动剂作用下,G蛋白偶联受体(GPCRs)能够激活G蛋白的α亚基,从而使Gα亚基与Gβγ亚基分离,被激活的Gα亚基通过信号转导进一步参与细胞的生理过程。但是,最新研究发现GPCRs和G蛋白存在多种偶联关系,GPCRs不仅能够激活Gα亚基,还可以与Gβγ亚基相互靠近,甚至会使G蛋白亚基构象发生重排而不分离,这对于疾病发病机制的研究及新的药物靶点的发现具有重要意义。就GPCRs与G蛋白之间的相互作用以及最新研究技术作一简要综述。

The interaction of G protein-coupled receptors （GPCRs） and G protein is an important part of signal transduction. Traditionally, GPCRs are able to activate Gα subunit following agonist stimulation, resulting in the dissociation of Gα subunit and Gβγ subunit. Activated Gα then participates in the physiological processes of cells. However, recent researches reveal there are multiple coupling relationships between GPCRs and G protein. GPCRs can interact with different subtypes of Gα and get close to Gβγ subunit. Even more, it was reported that activation of some heterotrimeric G proteins may trigger subunit rearrangement instead of dissociation of subunits, which is of great significance for researching the pathogenesis of disease and discovering new drug targets. In this paper, we review the interaction between GPCRs and G protein and the last research techniques.