Alfaras-Melainis Konstantinos, Gomes Ivone, Rozenfeld Raphael, Zachariou Venetia, Devi Lakshmi
Department of Pharmacology and Systems Therapeutics, Mount Sinai School of Medicine, New York, NY, USA.
Front Biosci (Landmark Ed). 2009 Jan 1;14(9):3594-607. doi: 10.2741/3474.
Opioid receptors, MORP, DORP and KORP, belong to the family A of G protein coupled receptors (GPCR), and have been found to modulate a large number of physiological functions, including mood, stress, appetite, nociception and immune responses. Exogenously applied opioid alkaloids produce analgesia, hedonia and addiction. Addiction is linked to alterations in function and responsiveness of all three opioid receptors in the brain. Over the last few years, a large number of studies identified protein-protein interactions that play an essential role in opioid receptor function and responsiveness. Here, we summarize interactions shown to affect receptor biogenesis and trafficking, as well as those affecting signal transduction events following receptor activation. This article also examines protein interactions modulating the rate of receptor endocytosis and degradation, events that play a major role in opiate analgesia. Like several other GPCRs, opioid receptors may form homo or heterodimers. The last part of this review summarizes recent knowledge on proteins known to affect opioid receptor dimerization.
阿片受体，即μ阿片受体（MORP）、δ阿片受体（DORP）和κ阿片受体（KORP），属于G蛋白偶联受体（GPCR）A家族，已发现其可调节大量生理功能，包括情绪、应激、食欲、痛觉感受和免疫反应。外源性应用阿片生物碱可产生镇痛、欣快感和成瘾性。成瘾与大脑中所有三种阿片受体的功能和反应性改变有关。在过去几年中，大量研究确定了在阿片受体功能和反应性中起重要作用的蛋白质-蛋白质相互作用。在此，我们总结了已显示影响受体生物发生和运输的相互作用，以及影响受体激活后信号转导事件的相互作用。本文还研究了调节受体内吞作用和降解速率的蛋白质相互作用，这些事件在阿片类镇痛中起主要作用。与其他几种GPCR一样，阿片受体可能形成同二聚体或异二聚体。本综述的最后一部分总结了关于已知影响阿片受体二聚化的蛋白质的最新知识。
