可药性
α-突触核蛋白
蛋白质聚集
小分子
肽
脂锚定蛋白
化学
生物化学
血浆蛋白结合
细胞生物学
功能(生物学)
多巴胺能
共核细胞病
蛋白质-蛋白质相互作用
生物物理学
生物
帕金森病
疾病
多巴胺
神经科学
医学
自噬
病理
细胞凋亡
基因
作者
Richard M. Meade,Scott G. Allen,Christopher Williams,Tingting Tang,Matthew P. Crump,Jody M. Mason
标识
DOI:10.1016/j.xcrp.2023.101563
摘要
Misfolding and aggregation of alpha-synuclein (αS) into toxic conformations is involved in numerous neurodegenerative diseases. In Parkinson’s disease (PD), this occurs within dopaminergic neurons, causing cell death and disease symptoms. During αS aggregation, many protein-protein interactions (PPIs) form over broad and flat protein surfaces, limiting potential for small-molecule intervention. Peptides, however, harbor great therapeutic promise since they can selectively engage with and modulate the large surface areas involved yet are small enough to function as druggable agents if suitably structured. Here, we explore the first 25 residues of αS (αS1–25) as a template for peptide-based αS aggregation antagonists. We report that αS1–25 inhibits lipid-induced αS aggregation in a dose-dependent manner. αS1–25 functions by binding to lipids to prevent αS binding, with both αS and peptide requiring lipid for inhibition to occur. These findings present a potential mechanistic route for the treatment or prevention of PD.
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