C 族GPCRs 寡聚体的激活机制

C族GPCRs是体内重要的受体亚家族,参与众多重要的生理和病理进程。该族受体的单体包含七螺旋跨膜结构(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)、C末端等多个功能域,同时形成组成性的二聚体和寡聚体。这种多功能域寡聚体结构使该家族受体的激活机制非常复杂,本文回顾和介绍了多年以来对该家族受体在单体、二聚体、寡聚体等多个层面的激活机制研究的历程和进展,同时也展望了进一步的研究方向和这些研究成果对于开发新型药物的意义。

The activation mechanism of Class C GPCRs oligomer

Class C GPCRs are important receptors sub-family and involved in many physiologic and pathologic processes in vivo.The monomer of these receptor is composed of transmembrane HD(heptahelical transmembrane domain),extracellular VFT(venus flytrap domain),CRD(cysteine-rich domain) which between in VFT and CRD and intracellular C-tail.In the other hand,these receptors could form constitutive and exclusive homodimer or heterodimer,and some members of them could also form high order oligomer.So the complex structure of these receptor provide a complicated activation mechanism.In this paper,we reviewed the course and advance of the research of activation mechanism of these receptors in different level included monomer,dimer and tetramer.Lastly we also point the next research in this field and the significance and new insights of these researches to discover new drug.