Instituto de Investigaciones Bioquímicas de Bahía Blanca, Departamento de Biología, Bioquímica y Farmacia, Universidad Nacional del Sur-Consejo Nacional de Investigaciones Científicas Y Técnicas (CONICET), Camino La Carrindanga Km 7-8000, Bahía Blanca, Argentina.
Centre for Computational Chemistry, School of Chemistry, University of Bristol, Bristol, BS8 1TS, UK.
Mol Neurobiol. 2022 Oct;59(10):6076-6090. doi: 10.1007/s12035-022-02947-8. Epub 2022 Jul 20.
The α7 nicotinic acetylcholine receptor (nAChR) is present in neuronal and non-neuronal cells and has anti-inflammatory actions. Molecular dynamics simulations suggested that α7 nAChR interacts with a region of the SARS-CoV-2 spike protein (S), and a potential contribution of nAChRs to COVID-19 pathophysiology has been proposed. We applied whole-cell and single-channel recordings to determine whether a peptide corresponding to the Y674-R685 region of the S protein can directly affect α7 nAChR function. The S fragment exerts a dual effect on α7. It activates α7 nAChRs in the presence of positive allosteric modulators, in line with our previous molecular dynamics simulations showing favourable binding of this accessible region of the S protein to the nAChR agonist binding site. The S fragment also exerts a negative modulation of α7, which is evidenced by a profound concentration-dependent decrease in the durations of openings and activation episodes of potentiated channels and in the amplitude of macroscopic responses elicited by ACh. Our study identifies a potential functional interaction between α7 nAChR and a region of the S protein, thus providing molecular foundations for further exploring the involvement of nAChRs in COVID-19 pathophysiology.
α7 型烟碱型乙酰胆碱受体(nAChR)存在于神经元和非神经元细胞中,具有抗炎作用。分子动力学模拟表明,α7 nAChR 与 SARS-CoV-2 刺突蛋白(S)的一个区域相互作用,并且已经提出 nAChRs 可能对 COVID-19 病理生理学有贡献。我们应用全细胞和单通道记录来确定 S 蛋白的 Y674-R685 区域对应的肽是否可以直接影响 α7 nAChR 功能。S 片段对 α7 具有双重作用。它在正变构调节剂存在下激活 α7 nAChRs,这与我们之前的分子动力学模拟结果一致,表明 S 蛋白的这个可及区域与烟碱型乙酰胆碱受体激动剂结合位点有良好的结合。S 片段还对 α7 产生负调节作用,这表现在增强通道的开放和激活事件的持续时间以及 ACh 诱发的宏观反应幅度随着浓度的增加而明显减少。我们的研究确定了 α7 nAChR 和 S 蛋白的一个区域之间的潜在功能相互作用,从而为进一步探索 nAChRs 在 COVID-19 病理生理学中的作用提供了分子基础。