大麻素受体二聚化及其激活机理

Mechanism of dimerization and activation of CB_1and CB_2 receptor

大麻素受体1（cannabinoid receptor 1,CB1）和大麻素受体2（cannabinoid receptor 2,CB_2）可以形成同源二聚体,也可以与多种受体形成异源二聚体。异源二聚体大大增加了G蛋白偶联受体（G proteincoupled receptors,GPCRs）功能反应的范畴,对药物的开发存在很大的潜力。异源二聚体具有不同于单体和同源二聚体的高阶结构特点[1],CB1受体。

Cannabinoid receptor 1（ CB1） and cannabinoid receptor 2（ CB_2） are important members of G protein-coupled receptors（ GPCRs）. Numerous studies have shown that CB_1 receptor can form heterodimers with dopamine receptors（ D2）,μ-opioid receptor（ μOR）,orexin-1 receptor,adenosine receptor（ A_（2A）） or β2 adrenergic receptors,and then forming an essential functional entity. This review summarizes the research progress on heterodimers of cannabinoid CB1 or CB_2,the function of heterodimers as well as the downstream signalings. The different pharmacological properties of the receptor heterodimer lead to bringing a change in receptor pharmacology,which will have a profound impact on drug development.