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原子模拟揭示错义突变对 SynGAP1 结构和功能的影响。

Atomistic simulations reveal impacts of missense mutations on the structure and function of SynGAP1.

机构信息

MedChem.fi, Institute of Biomedicine, Integrative Physiology and Pharmacology, University of Turku, FI-20014 Turku, Finland.

InFLAMES Research Flagship, University of Turku, 20014 Turku, Finland.

出版信息

Brief Bioinform. 2024 Sep 23;25(6). doi: 10.1093/bib/bbae458.

Abstract

De novo mutations in the synaptic GTPase activating protein (SynGAP) are associated with neurological disorders like intellectual disability, epilepsy, and autism. SynGAP is also implicated in Alzheimer's disease and cancer. Although pathogenic variants are highly penetrant in neurodevelopmental conditions, a substantial number of them are caused by missense mutations that are difficult to diagnose. Hence, in silico mutagenesis was performed for probing the missense effects within the N-terminal region of SynGAP structure. Through extensive molecular dynamics simulations, encompassing three 150-ns replicates for 211 variants, the impact of missense mutations on the protein fold was assessed. The effect of the mutations on the folding stability was also quantitatively assessed using free energy calculations. The mutations were categorized as potentially pathogenic or benign based on their structural impacts. Finally, the study introduces wild-type-SynGAP in complex with RasGTPase at the inner membrane, while considering the potential effects of mutations on these key interactions. This study provides structural perspective to the clinical assessment of SynGAP missense variants and lays the foundation for future structure-based drug discovery.

摘要

突触 GTP 酶激活蛋白(SynGAP)中的从头突变与神经发育障碍有关,如智力障碍、癫痫和自闭症。SynGAP 也与阿尔茨海默病和癌症有关。尽管致病性变异在神经发育障碍中具有高度外显率,但其中相当一部分是由难以诊断的错义突变引起的。因此,进行了基于计算机的诱变,以探究 SynGAP 结构中 N 端区域的错义效应。通过广泛的分子动力学模拟,涵盖了 211 个变体的三个 150-ns 重复,评估了错义突变对蛋白质折叠的影响。还使用自由能计算定量评估了突变对折叠稳定性的影响。根据结构影响将突变分为潜在致病性或良性。最后,该研究在考虑突变对这些关键相互作用的潜在影响的情况下,将野生型-SynGAP 与内在膜上的 RasGTPase 复合物,为未来基于结构的药物发现奠定了基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ac4/11418247/16d26d9247b4/bbae458f1.jpg

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