《生命科学》 2015, 27(4): 445-452

G蛋白偶联受体的结构与功能研究进展

程建昕，唐　赟*

(华东理工大学药学院上海市新药设计重点实验室，上海 200237)

摘　要：摘　要：G 蛋白偶联受体(GPCR) 是一类具有七个跨膜螺旋结构的超家族，参与机体内许多重要的生物学信号转导过程，其功能异常将引起一系列疾病的发生，因而是一类十分重要的药物作用靶标。近几年来，研究人员在GPCR 的三维结构测定方面取得了一系列重要的研究进展，这些突破性成就不仅将GPCR 家族各亚型及成员的基本结构特征清晰地呈现给人们，也促使人们对它们的功能展开了新一轮广泛而深入的探索。这为基于结构的药物设计，如具有功能选择性的变构调节剂等新型配体的设计，提供了大量重要的信息。现对最近两年在GPCR 结构和功能研究方面所取得的重要进展进行综述，并对基于GPCR 结构的药物设计及进一步研究进行了展望。

Research advances in structures and functions of G protein-coupled receptors

CHENG Jian-Xin， TANG Yun*

(Shanghai Key Laboratory of New Drug Design， School of Pharmacy，
    East China University of Science and Technology， Shanghai 200237， China)

Abstract: Abstract: G protein-coupled receptors (GPCR) are a family of proteins containing seven transmembrane helixes， which participate in response to a wide range of intracellular signaling transduction. Because the dysfunction of GPCR will cause a series of disorders or diseases， they are extremely important drug targets. In recent years， a series of big advances in the determination of three-dimensional structures of GPCR has been made. These breakthroughs not only allow to clearly understand the basic structural characteristics of each GPCR subtype and individual members， but also prompt to launch a new round of broad and in-depth exploration on GPCR functions. All above-mentioned progresses greatly facilitate drug design based on GPCR structures， such as the design of new types of ligands with functional selectivity like allosteric modulators. In this review， we mainly summarized important advances achieved in aspects of GPCR structures and functions in recent two years. GPCR structure-based drug design and further research prospects were also reviewed.