Hansel Catherine S, Lanne Alice, Rowlands Hannah, Shaw Joseph, Collier Matthew J, Plant Helen
High-throughput Screening, Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Alderley Park, UK.
High-throughput Screening, Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Alderley Park, UK.
SLAS Technol. 2023 Dec;28(6):411-415. doi: 10.1016/j.slast.2023.08.004. Epub 2023 Aug 19.
Biophysical affinity screening is increasingly being adopted as a high-throughput hit finding technique in drug discovery. Automation is highly beneficial to high-throughput screening (HTS) since a large number of compounds need to be reproducibly tested against a biological target. Herein, we describe how we have automated two biophysical affinity screening methods that rely on a thermal shift in protein melting temperature upon small molecule binding: differential scanning fluorimetry (DSF) and the cellular thermal shift assay (CETSA).
生物物理亲和力筛选作为一种高通量的先导化合物发现技术，在药物研发中越来越受到广泛应用。自动化对高通量筛选（HTS）非常有益，因为需要对大量化合物针对生物靶点进行可重复测试。在此，我们描述了如何将两种基于小分子结合导致蛋白质解链温度发生热变化的生物物理亲和力筛选方法自动化：差示扫描荧光法（DSF）和细胞热位移分析（CETSA）。
