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C族GPCRs是体内重要的受体,参与众多重要的生理和病理进程,并具有复杂的结构和激活机制。在体内该族受体形成组成性的二聚体并具有七螺旋跨膜结构(heptahelical transmembrane domain,HD)、捕蝇草模块(venus flytrap domain,VFT)和半胱氨酸富集区(cysteine-rich domain,CRD)。本文系统介绍了近年来CRD单体的序列和结构解析,以及参与受体激活过程的机制研究的历程和进展。同时也展望了这些基础研究成果对于开发新的更具有成药性的以C族GPCRs为靶点的变构剂的指导意义。
C family of GPCRs is an important receptor in vivo, involved in many important physiological and pathological processes, and has a complex structure and activation mechanism. This family of receptors forms constitutive dimers in vivo and has the function of heptahelical transmembrane domain (HD), venus flytrap domain (VFT) and cysteine- rich domain, CRD). This article systematically introduced the sequence and structure analysis of CRD monomer in recent years, as well as the mechanism and progress of the receptor activation process. At the same time, these basic research findings are also expected to guide the development of new and more drug-specific allosteric agents targeting Group C GPCRs.