G蛋白偶联受体(G protein-coupled receptor, GPCR)在细胞信号传导过程中发挥关键作用，其三维结构的解析对于深入理解GPCR的结构与功能关系具有重要意义。2000年以前，GPCR的高分辨率结构解析一直是困扰科学家们的一个难题。近年来，GPCR的结构生物学研究实现了飞跃式的发展。本文简要综述了GPCR结构解析的方法与创新点，并以CCR5和P2Y1R两种受体的结构解析为例阐述GPCR结构对于功能研究和药物研发的重要性。

G protein-coupled receptors (GPCRs) play key roles in cell signal transduction. GPCR structures are important for understanding structure-functional relationship of the GPCR superfamily. Before the year 2000, the high-resolution GPCR structure is one of the major obstacles in structural biology field. In recent years, the structural studies of GPCRs have been developed remarkably. Here, we briefly summarize the methods used in GPCR structure determination, and also take the CCR5 and P2Y1R structures as examples to discuss the significance of GPCR structures on functional studies and drug discovery.