g蛋白偶联受体失敏的分子机制 - 湖南师范大学.pdfVIP

7 1 生命科学研究 Vol.7 No. 1 20033 Life Science Research Mar. 2003 G 1 2 1 肖贞良 , 夏前明, 钱桂生 ( 1. , 400037; 2. , 610083) : 蛋白偶联受体( PCRs) 受到激动剂持续刺激时易发生失 .受体内化是 PCRs 失 重要分子机制. PCRs在 蛋白偶联受体激酶( RKs)第二信使调节激酶等作用下发生磷酸化, 磷酸化的 PCRs 与抑制蛋白 ( arrestins) 结合后导致受体与 蛋白失偶联,并通过胞吞由细胞膜表面向膜内转移, 从而因 PCRs 的内化而表 现为失 . : 失 ; 蛋白偶联受体;磷酸化; 内化;胞吞 : Q372;R363 : A : 1007-7847(2003)01-0015-05 Molecular Mechanism of G Protein-coupled Receptors Desensitization XIAO Zhen-liang,XIA Qian-ming,QIAN u-i sheng ( 1. Department of Respiratory Diseases , Xinqiao Hospital , Third Military Medical University , Chongqing 400037, China; 2. Department of Respiratory Diseases , ChengduArmy General Hospital, Chengdu 610083, Shichuan, China) Abstract: Desensitization may occur in protein-coupled receptors( PCRs) when agonists exist continuously.In- ternalization is an important mechanism of PCRs desensitization.Phosphorylation of PCRs happens under the ac- tion of protein-coupled receptor kinases( RKs) or the second messenger dependent kinases.The combination of phosphorylated RCPs and arrestins leadsto the decoupling of RCPswith protein,then RCPs transfer to the in- ternal surface of cell membrane and thus desensitization of RCPs occurs. Key words: desensitazation; protein-coupled receptor;phosphorylization; internalization; endocytosis ( fi e Science Research ,2003,7( 1) :015~ 019) ( protein-coupled receptor, 1 GPCRs PCRs) . PCRs 5- , PCRs ,