GPCR-Gα融合蛋白及其在oGPCRs配基筛选中的应用  

GPCR-Gα fusion protein and its applications on ligand screening of orphan G protein-coupled receptors

作　　者：吴芳明[1] 刘永学[2] 

机构地区：[1]江西中医学院中药系,江西南昌330004 [2]军事医学科学院放射医学研究所药理毒理室,北京100850

出　　处：《中国药理学通报》2005年第5期518-521,共4页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No30171096);全军医药卫生"十五"面上资助项目(No01MB056)

摘　　要：GPCRGα融合蛋白是近几年用于受体研究的新颖手段之一,它的表达确保了受体与G蛋白之间1∶1的化学计量关系、空间位置上的邻近性及适宜于高通量的配基筛选,使其为孤儿G蛋白偶联受体提供了一种新的研究策略,将在孤儿受体的配基筛选中发挥重要作用,对研发以oGPCR为作用靶点的新药产生积极意义。GPCR-G alpha fusion protein has been used to investig ate receptors in recent years. The expression of GPCR-G alpha fusion protein en sured defined 1∶1 stoichiometry, the physical proximity of GPCR to G alpha subu nit, and was suitable for high-throughput ligand screening. The fusion protein technology provided a novel strategy to study orphan GPCRs. Obviously, it will p lay important roles in ligand screening of the orphan GPCRs and exert its signif icances in the R&D of novel drugs targeted at oGPCRs.

关 键 词：孤儿G蛋白偶联受体 G蛋白 融合蛋白 配基筛选 

分 类 号：R-05[医药卫生] R392.11