G蛋白偶联受体 (GPCRs) ,是体内最大的蛋白质超家族。 GPCRs的基本结构已清楚 ,但高分辨率的三维结构还未得到。根据结构的同源性 ,GPCRs主要分为 A、B、C3族。GPCRs配体的多样性决定配体结合域的多样性。受体分子内相互作用力的破坏 ,质子化 ,构象变化 ,与 G蛋白的偶联以及受体二聚化参与了 GPCRs的活化过程。 GPCRs的活化模式有 3种 :二态模式、多态模式和顺序结合和构象选择模式。 G-protein coupled receptors (GPCRs), the largest protein superfamily in the body. The basic structure of GPCRs is clear, but high-resolution three-dimensional structures have not been obtained yet. According to the structural homology, GPCRs are mainly divided into A, B and C3 families. The diversity of GPCRs ligands determines the diversity of ligand binding domains. The destruction of the intramolecular interaction force, the protonation, the conformational change, the coupling with G protein and the receptor dimerization are involved in the activation of GPCRs. There are three types of activation of GPCRs: two-state mode, multi-state mode and sequence combination and conformational selection mode.