中文摘要：

不同类型G蛋白偶联受体（GPCRs）之间的异源二聚化作用已得到普遍认可，异源二聚体具有不同于单体和同源二聚体的高阶结构特点，这在一定层次上类似于变构调节机制，使得GPCRs异源二聚体呈现更高的信号特异性和多样性。成功筛选GPCRs异源二聚体的特异配体或偏向性配体，能够为研发降低副作用的药物提供新的策略。该文就GPCRs异源二聚体的信号特点及其偏向性配体的生理药理学价值和筛选GPCRs异源二聚体偏向性配体的技术做一简要综述。

英文摘要：

The receptor heteromerization involving different G- protein-coupled receptors （GPCRs） is now an established phe- nomenon. The relevance of higher order structures of GPCR het- erodimers has been demonstrated compared with monomers/homodimers of the respective constituent receptor units, which pro- vides an allosteric modulative meehanism to achieve greater sig- nal diversity and specificity. The concepts of heteromerization and heterodimer-selective/biased ligands introduce exciting opportunities for enhancing signal specificity and therefore have the potential to play a crucial role in future drug discovery. There- fore, this article mainly reviews the signal transduction property of heterodimers, pharmacological effects of their biased ligands and the new research technologies.