中文摘要：

G蛋白偶联受体（GPCR）是当今药物治疗中最有效靶向作用的受体超家族之一,它在人类的正常生理状态和疾病过程中都发挥着极大的功效。近年研究发现,GPCR脱敏作用的调节器β-arrestin,可作为真正的衔接蛋白将信号转导到多重效应途径。β-arrestin介导的信号对生化和功能方面的影响力都不同于传统G蛋白介导的信号。由此发现辨别出的多种G蛋白-偏向配体或β-arrestin偏向配体,不仅是用来研究GPCR信号生化特征的有效工具,还具有被开发成治疗药物的潜力。因此,该文就偏向性配体的特点、作用机制、药理学作用及研究偏向性配体的技术进行综述。

英文摘要：

G protein-coupled receptor（GPCR）,superfamily represent some of the most successful targets of modern drug therapy,with proven significant efficacy in a broad range of human conditions and disease processes.It has recently been appreciated that β-arrestins,once viewed simply as regulators of GPCR desensitization,act as multifunctional adapter proteins that mediate distinct intracellular signals.Moreover,β-arrestin-mediated signaling has distinct functional and biochemical consequences from that mediated by G proteins.With the discovery of β-arrestin-mediated signaling has come a new appreciation of G protein-and β-arrestin-biased ligans.These ligands are not only useful tools for investigating the biochemistry of GPCR signalling,they also have the potential to be developed into new classes of therapeutics.Therefore,this article will mainly review the property,mechanism,pharmacological effects of biased ligands and the new research technologies.