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非瑟酮对超氧化物歧化酶1 E100K突变体聚集过程的抑制作用:基于计算机的药物设计作为肌萎缩侧索硬化症的潜在治疗方法。

Inhibitory effect of Fisetin against the aggregation process of SOD1 E100K mutant: computer-based drug design as a potential therapeutic for ALS disease.

作者信息

Seyedi Asl Fatemeh Sadat, Malverdi Nasrin, Ataei Kachouei Fatemeh Sadat, Zarei Fatemeh, Ghiabi Shamim, Baziyar Payam, Nabi-Afjadi Mohsen

机构信息

Medical School, Tehran University of Medical Sciences, Tehran, Iran.

Department of Cell and Molecular Biology and Microbiology, Faculty of Biological Science and Technology, University of Isfahan, Isfahan, Iran.

出版信息

Front Chem. 2025 May 22;13:1569777. doi: 10.3389/fchem.2025.1569777. eCollection 2025.

Abstract

Protein misfolding and aggregation in superoxide dismutase 1 (SOD1) are linked to the neurodegenerative disease amyotrophic lateral sclerosis (ALS). SOD1 mutations have a significant role in the pathophysiology and fast behavior of protopathic proteins in ALS illness. The E100K mutation may be useful in uncovering the pathogenic mechanism of SOD1 associated with ALS. According to several studies, giving small molecule inhibitors made from polyphenolic flavonoid compounds may be a viable treatment strategy for neurological conditions. Using molecular docking and MD simulations, we have identified a potential flavonoid drug that may successfully inhibit SOD1's amyloidogenic activity. Puerarin, Fisetin, and Peonidin provided intriguing pharmacological hints during the initial screening of flavonoids. The Fisetin-E100K complex had a larger residual energy contribution and substantial binding than other flavonoid compounds. The findings showed that, unlike other materials, Fisetin increased the structural stability, hydrophobicity, and flexibility of the mutant while reducing the amount of β-sheets. Furthermore, to distinguish aggregation in the mutant (unbound/bound) states, we displayed modifications in the free energy landscape (FEL). As a result, Fisetin was identified as having therapeutic potential against the E100K, which might make it a viable pharmacological option for the creation of inhibitors that lower the chance of ALS death.

摘要

超氧化物歧化酶1(SOD1)中的蛋白质错误折叠和聚集与神经退行性疾病肌萎缩侧索硬化症(ALS)相关。SOD1突变在ALS疾病中原发性蛋白质的病理生理学和快速行为中起重要作用。E100K突变可能有助于揭示与ALS相关的SOD1的致病机制。根据多项研究,给予由多酚类黄酮化合物制成的小分子抑制剂可能是治疗神经系统疾病的一种可行策略。通过分子对接和分子动力学模拟,我们确定了一种潜在的黄酮类药物,它可能成功抑制SOD1的淀粉样蛋白生成活性。在黄酮类化合物的初步筛选过程中,葛根素、非瑟酮和芍药色素提供了有趣的药理学线索。与其他黄酮类化合物相比,非瑟酮 - E100K复合物具有更大的剩余能量贡献和更强的结合力。研究结果表明,与其他物质不同,非瑟酮增加了突变体的结构稳定性、疏水性和柔韧性,同时减少了β - 折叠的数量。此外,为了区分突变体(未结合/结合)状态下的聚集情况,我们展示了自由能景观(FEL)的变化。因此,非瑟酮被确定具有针对E100K的治疗潜力,这可能使其成为开发降低ALS死亡几率的抑制剂的一种可行的药理学选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4677/12138904/cdae8a99aea6/fchem-13-1569777-g001.jpg

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