【摘要】 G蛋白偶联受体(G protein-coupled receptor,GPCR)是一个重要的细胞膜受体超家族。β-arrestin 1和β-ar-restin 2是广泛存在于细胞内的调配器和支架蛋白,它们在G蛋白偶联受体的细胞内信号转导、脱敏、内化、复敏以及G蛋白非依赖的信号转导中发挥重要作用。生物发光共振能量转移(BRET)技术能够实时监测活细胞内GPCRs和β-arrestins的相互作用,可进一步阐明β-arrestin调节GPCRs的作用机制,有助于开发新一代影响GPCRs功能活动的药物。更多还原

【Abstract】 G protein-coupled receptors constitute an important super family of cell surface proteins.β-arrestin 1and 2 are widely expressed intracellular adaptor and scaffolding proteins playing important roles in G protein-coupled receptor desensitization,internalization,intracellular trafficking,and G protein-independent signaling.Recent development in bioluminescence resonance energy transfer(BRET)technology makes it possible to monitor the GPCR-β-arrestin complexes in live cells in a real-time manner;and investigators can further elucidate the ever-expanding roles ofβ-arrestins in mediating GPCR function,which will help to develop the new generation of drugs targeting GPCRs.更多还原