C族GPCRs的半胱氨酸富集区的研究进展及药学意义  

Recent Research and its Pharmacologic Significance on Cysteine-Rich Domain of Class C GPCRs

作　　者：阮嫔[1] 赵菡[2] 薛礼[2] 蒋明[2] 黄思罗[1] 

机构地区：[1]湖北医药学院附属东风总医院药剂部,湖北十堰442008 [2]华中科技大学生命科学与技术学院,分子生物物理教育部重点实验室,湖北武汉430074

出　　处：《现代生物医学进展》2012年第9期1755-1759,共5页Progress in Modern Biomedicine

基　　金：第47批中国博士后面上基金(20100471184);国家自然科学面上基金(30973514;31100548)

摘　　要：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。Class C GPCRs are important receptors in vivo and involved in many physiologic and pathologic process.These receptors have complex structure and active mechanism.They are constitutive dimer and each monomer is composed of transmembrane HD（heptahelical transmembrane domain）,extracellular VFT（venus flytrap domain） and CRD（cysteine-rich domain） which between in VFT and CRD.Although there are many results in the activation mechanism of these receptors,but until recently the role of CRD in the activation process is largely unknown.So we reviewed the course and advance of the research in the sequence,structure,function,and their conformation change in the activation process of these receptor dimmers.And lastly we also point the significance and new insights of the Class C GPCR based-drug discovery to gain the new allosteric modulators which have better clinic implication..

关 键 词：C族G蛋白偶联受体 CRD 激活机制 构象变化 

分 类 号：Q25[生物学—细胞生物学] Q27