Department of Pharmacology-Physiology, Université de Sherbrooke, Centre de Recherche du CHUS, Sherbrooke, QC, Canada; Quebec Pain Research Network, Sherbrooke, QC, Canada.
College of Medicine, Member of QU Health, Qatar University, Doha, Qatar.
Vitam Horm. 2019;111:49-90. doi: 10.1016/bs.vh.2019.06.001. Epub 2019 Jul 8.
The delta opioid receptor (DOP) belongs to the Class A, rhodopsin-like family of G protein-coupled receptors. Although this receptor has a high level of similarity with the other opioid receptors, it displays unique aspects and functions. Indeed, as opposed to most membrane receptors, DOP is poorly addressed to the plasma membrane. In this chapter, we first review the molecular and cellular mechanisms regulating the expression and the cellular trafficking/sorting of DOP. We then summarize the structural insights of this receptor through the analysis of the existing crystal structures, with a particular focus on the role of the sodium binding site. Finally, we review the current signaling mechanisms mediating receptor function and desensitization.
德尔塔阿片受体(DOP)属于 A 类,视紫红质样 G 蛋白偶联受体家族。尽管该受体与其他阿片受体具有高度相似性,但它表现出独特的方面和功能。事实上,与大多数膜受体不同,DOP 不易被定位到质膜上。在本章中,我们首先综述了调节 DOP 表达和细胞内运输/分拣的分子和细胞机制。然后,我们通过分析现有的晶体结构来总结该受体的结构见解,特别关注钠离子结合位点的作用。最后,我们综述了介导受体功能和脱敏的当前信号转导机制。