一种用于筛选淀粉样β结合化合物的稳健且可扩展的高通量兼容测定法。
A Robust and Scalable High-Throughput Compatible Assay for Screening Amyloid-β-Binding Compounds.
机构信息
Vanderbilt University Institute of Imaging Science, Vanderbilt University, Nashville, TN, USA.
Vanderbilt High-Throughput Screening Facility, Nashville, TN, USA.
出版信息
J Alzheimers Dis. 2019;70(1):187-197. doi: 10.3233/JAD-190316.
Abstract
A robust fluorescent readout assay using topologically-sensitive dyes improves the screening of novel amyloid-binding molecules. One of the key components that make this assay more realistic is the use of endogenous amyloid obtained from 5XFAD mouse brains. The assay conditions were optimized for high throughput screening operation with Z-prime values >0.6. Using a combination of library of 3,500 compounds including known drugs, natural-derived molecules and random organic molecules, 8 unique molecules were identified as potential amyloid-binding agents.
摘要
一种使用拓扑敏感染料的稳健荧光读出测定法提高了新型淀粉样蛋白结合分子的筛选效率。使该测定法更接近实际情况的关键因素之一是使用源自 5XFAD 小鼠大脑的内源性淀粉样蛋白。测定法条件经过优化，可实现高通量筛选操作，Z' 值>0.6。通过组合使用包括已知药物、天然衍生分子和随机有机分子在内的 3500 种化合物文库，鉴定出 8 种独特的分子作为潜在的淀粉样蛋白结合剂。
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