An Economical High-Throughput "FP-Tag" Assay for Screening Glycosyltransferase Inhibitors
An Economical High-Throughput "FP-Tag" Assay for Screening Glycosyltransferase Inhibitors
复制标题
用于筛选糖基转移酶抑制剂的经济高效高通量 FP 标签测定法
DOI：
10.1002/cbic.202000746
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发表时间：
2021-01-21
期刊：
影响因子：
3.2
通讯作者：
Gao, Zhizeng
中科院分区：
文献类型：
--
作者：
Yin, Xinjian;Li, Jiaxin;Gao, Zhizeng
O-GlcNAc转移酶(OGT)参与多种细胞过程，选择性OGT抑制剂是研究O-GlcN酰化功能的有价值的工具，并有可能导致治疗。然而，适用于大规模HTS的高通量OGT分析仍然缺乏能够识别同时针对受体、供体和变构结合位点的抑制剂。在这里，我们报告了一种高通量的牛血清白蛋白(BSA)作为一种低成本和高质量的“FP-Tag”OGT分析方法的发展。结果表明，2-甲基黄体酮是一种低微摩尔的OGT抑制剂。这种以牛血清白蛋白为“FP-Tag”的检测方法将在其他糖基转移酶中得到更多的应用。
O-GlcNAc transferase (OGT) is involved in many cellular processes, and selective OGT inhibitors are valuable tools to investigate O-GlcNAcylation functions, and could potentially lead to therapeutics. However, high-throughput OGT assays that are suitable for large-scale HTS and can identify inhibitors targeting both acceptor, donor sites, and allosteric binding-sites are still lacking. Here, we report the development of a high-throughput "FP-Tag" OGT assay with bovine serum albumin (BSA) as a low-cost and superior "FP-Tag". With this assay, 2-methyleurotinone was identified as a low-micromolar OGT inhibitor. This type of assay with BSA as "FP-Tag" would find more applications with other glycosyltransferases.