Gonzalez-Lozano Miguel A, Wortel Joke, van der Loo Rolinka J, van Weering Jan R T, Smit August B, Li Ka Wan
Center for Neurogenomics and Cognitive Research, Department of Molecular and Cellular Neurobiology, Amsterdam Neuroscience, Vrije Universiteit Amsterdam, 1081 Amsterdam, The Netherlands.
Center for Neurogenomics and Cognitive Research, Department of Functional Genomics, Amsterdam Neuroscience, Vrije Universiteit Amsterdam, 1081 Amsterdam, The Netherlands.
Cells. 2021 Jun 2;10(6):1375. doi: 10.3390/cells10061375.
The metabotropic glutamate receptor 5 (mGluR5) is an essential modulator of synaptic plasticity, learning and memory; whereas in pathological conditions, it is an acknowledged therapeutic target that has been implicated in multiple brain disorders. Despite robust pre-clinical data, mGluR5 antagonists failed in several clinical trials, highlighting the need for a better understanding of the mechanisms underlying mGluR5 function. In this study, we dissected the molecular synaptic modulation mediated by mGluR5 using genetic and pharmacological mouse models to chronically and acutely reduce mGluR5 activity. We found that next to dysregulation of synaptic proteins, the major regulation in protein expression in both models concerned specific processes in mitochondria, such as oxidative phosphorylation. Second, we observed morphological alterations in shape and area of specifically postsynaptic mitochondria in mGluR5 KO synapses using electron microscopy. Third, computational and biochemical assays suggested an increase of mitochondrial function in neurons, with increased level of NADP/H and oxidative damage in mGluR5 KO. Altogether, our observations provide diverse lines of evidence of the modulation of synaptic mitochondrial function by mGluR5. This connection suggests a role for mGluR5 as a mediator between synaptic activity and mitochondrial function, a finding which might be relevant for the improvement of the clinical potential of mGluR5.
代谢型谷氨酸受体5(mGluR5)是突触可塑性、学习和记忆的重要调节因子;而在病理状态下,它是一个公认的治疗靶点,与多种脑部疾病有关。尽管临床前数据充足,但mGluR5拮抗剂在多项临床试验中均告失败,这凸显了深入了解mGluR5功能背后机制的必要性。在本研究中,我们使用基因和药理学小鼠模型,通过长期和急性降低mGluR5活性,剖析了由mGluR5介导的分子突触调节。我们发现,除了突触蛋白失调外,两种模型中蛋白质表达的主要调节都涉及线粒体的特定过程,如氧化磷酸化。其次,我们使用电子显微镜观察到mGluR5基因敲除突触中特定突触后线粒体的形状和面积发生了形态学改变。第三,计算和生化分析表明,mGluR5基因敲除的神经元中线粒体功能增强,NADP/H水平升高且存在氧化损伤。总之,我们的观察结果提供了多条证据,证明mGluR5对突触线粒体功能具有调节作用。这种联系表明mGluR5作为突触活动和线粒体功能之间的介质发挥作用,这一发现可能与提高mGluR5的临床应用潜力相关。