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用于检测α-突触核蛋白聚集状态的小分子荧光探针。

Small molecule-based fluorescent probes for the detection of α-Synuclein aggregation states.

作者信息

Haque Rajibul, Maity Debabrata

机构信息

Department of Natural Products and Medicinal Chemistry, CSIR-Indian Institute of Chemical Technology (CSIR-IICT), Hyderabad 500007, India.

Department of Natural Products and Medicinal Chemistry, CSIR-Indian Institute of Chemical Technology (CSIR-IICT), Hyderabad 500007, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India.

出版信息

Bioorg Med Chem Lett. 2023 Apr 15;86:129257. doi: 10.1016/j.bmcl.2023.129257. Epub 2023 Mar 24.

Abstract

The formation of aggregates due to protein misfolding is encountered in various neurodegenerative diseases. α-Synuclein (α-Syn) aggregation is linked to Parkinson's disease (PD). It is one of the most prevalent neurodegenerative disorders after Alzheimer's disease. Aggregation of α-Syn is associated with Lewy body formation and degeneration of the dopaminergic neurons in the brain. These are the pathological hallmarks of PD progression. α-Syn aggregates in a multi-step process. The native unstructured α-Syn monomers combine to form oligomers, followed by amyloid fibrils, and finally Lewy bodies. Recent evidence suggests that α-Syn oligomerization and fibrils formation play major roles in PD development. α-Syn oligomeric species is the main contributor to neurotoxicity. Therefore, the detection of α-Syn oligomers and fibrils has drawn significant attention for potential diagnostic and therapeutic development. In this regard, the fluorescence strategy has become the most popular approach for following the protein aggregation process. Thioflavin T (ThT) is the most frequently used probe for monitoring amyloid kinetics. Unfortunately, it suffers from several significant drawbacks including the inability to detect neurotoxic oligomers. Researchers developed several small molecule-based advanced fluorescent probes compared to ThT for the detection/monitoring of α-Syn aggregates states. These are summarized here.

摘要

蛋白质错误折叠导致的聚集体形成在多种神经退行性疾病中都有出现。α-突触核蛋白(α-Syn)聚集与帕金森病(PD)相关。它是继阿尔茨海默病之后最常见的神经退行性疾病之一。α-Syn聚集与路易小体的形成以及大脑中多巴胺能神经元的退化有关。这些是PD进展的病理特征。α-Syn通过多步骤过程聚集。天然的无结构α-Syn单体结合形成寡聚体,随后形成淀粉样纤维,最终形成路易小体。最近的证据表明,α-Syn寡聚化和纤维形成在PD发展中起主要作用。α-Syn寡聚体是神经毒性的主要贡献者。因此,α-Syn寡聚体和纤维的检测对于潜在的诊断和治疗发展引起了极大关注。在这方面,荧光策略已成为跟踪蛋白质聚集过程最受欢迎的方法。硫黄素T(ThT)是监测淀粉样蛋白动力学最常用的探针。不幸的是,它存在几个重大缺点,包括无法检测神经毒性寡聚体。与ThT相比,研究人员开发了几种基于小分子的先进荧光探针用于检测/监测α-Syn聚集状态。在此进行总结。

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