摘要
G蛋白偶联受体(G Protein-Coupled Receptor,GPCR)是真核细胞膜表面受体家族中规模最大且种类最多的一类受体蛋白,常以单体、同型或异型二聚体等形式发挥作用,具有良好的成药性.最近的研究发现,GPCR多聚化有助于GPCR的表达、成熟,并影响其与配体互作以及下游信号转导等过程.本文综述了GPCR多聚体在蛋白分选、配体调节、信号转导和内化过程中的作用,以及在某些疾病发生发展中的病理与生理作用机制,并探讨了GPCR多聚体研究的技术方法、目前存在的问题和未来发展方向,这对研发靶向GPCR多聚体的药物具有重要意义.
Abstract
G protein-coupled receptor(GPCR)is the largest and most diverse receptor family in the cell membrane surface,which is also the most widely studied pharmacological target.GPCR can function as either monomers or polymers.Studies have shown that GPCR polymers are not only helpful for GPCR maturation,but also can increase the diversity of signal transduction.At the same time,the internalization process of GPCR has also been shown to be influenced by the multimeric structure.It can be said that the whole process,including the expression,maturation,ligand binding,signal transduction,and signal termination,is affected by the GPCR multimer structure.As a result,GPCR polymerization has become an increasingly attractive study as a potential target for the treatment of diseases.This paper summarizes the role and performance of GPCR polymers in the process of protein sorting,ligand regulation,signal transduction and internalization,and points out the problems in the research process of GPCR multimers,which is of great significance for the drug research of GPCR polymers.
维普
万方数据