CNR Institute of Neuroscience, 20854 Vedano al Lambro, Italy.
NeuroMi Milan Center for Neuroscience, University of Milano-Bicocca, 20126 Milan, Italy.
Molecules. 2023 Jan 27;28(3):1247. doi: 10.3390/molecules28031247.
α3β4 nicotinic acetylcholine receptors (nARs) are pentameric ligand-gated cation channels that function in peripheral tissue and in the peripheral and central nervous systems, where they are critical mediators of ganglionic synaptic transmission and modulators of reward-related behaviours. In the pentamer, two α3β4 subunit couples provide ligand-binding sites, and the fifth single (accessory) subunit (α3 or β4) regulates receptor trafficking from the endoplasmic reticulum to the cell surface. A number of rare missense variants of the human β4 subunit have recently been linked to nicotine dependence and/or sporadic amyotrophic lateral sclerosis, and altered responses to nicotine have been reported for these variants; however, it is unknown whether the effects of mutations depend on the subunit within the ligand-binding couples and/or on the fifth subunit. Here, by expressing single populations of pentameric receptors with fixed stoichiometry in cultured cells, we investigated the effect of β4 variants in the fifth position on the assembly and surface exposure of α3β4 nAChRs. The results demonstrate that the missense mutations in the accessory subunit alone, despite not affecting the assembly of α3β4 receptors, alter their trafficking and surface localisation. Thus, altered trafficking of an otherwise functional nAChR may underlie the pathogenic effects of these mutations.
α3β4 烟碱型乙酰胆碱受体 (nAR) 是五聚体配体门控阳离子通道,存在于外周组织以及外周和中枢神经系统中,在神经节突触传递中发挥关键作用,也是奖赏相关行为的调节剂。在五聚体中,两个 α3β4 亚基对提供配体结合位点,而第五个单一(辅助)亚基(α3 或 β4)调节受体从内质网到细胞表面的转运。最近,人类β4 亚基的一些罕见错义变体与尼古丁依赖和/或散发性肌萎缩侧索硬化症有关,并且这些变体对尼古丁的反应发生改变;然而,尚不清楚突变的影响是否取决于配体结合对中的亚基和/或第五个亚基。在这里,通过在培养的细胞中表达具有固定比例的单一五聚体受体群体,我们研究了第五位β4 变体对α3β4 nAChR 组装和表面暴露的影响。结果表明,尽管辅助亚基中的错义突变不影响α3β4 受体的组装,但会改变它们的转运和表面定位。因此,这些突变的致病作用可能源于功能正常的 nAChR 转运的改变。