测定硫氧还蛋白还原酶 1 不可逆抑制剂的方案。
Protocol for assaying irreversible inhibitors of thioredoxin reductase 1.
机构信息
School of Chemical Engineering, Ocean Technology and Life Science (CEOTLS) & Panjin Institute of Industrial Technology (PIIT), Dalian University of Technology, Panjin 124221, China.
School of Chemical Engineering, Ocean Technology and Life Science (CEOTLS) & Panjin Institute of Industrial Technology (PIIT), Dalian University of Technology, Panjin 124221, China.
出版信息
STAR Protoc. 2024 Sep 20;5(3):103235. doi: 10.1016/j.xpro.2024.103235. Epub 2024 Aug 7.
Selenoprotein thioredoxin reductase 1 (TXNRD1) is a promising therapeutic target, with several inhibitors reported to inhibit TXNRD1 activity. These inhibitors have the potential for applications such as anti-tumor medications. Here, we present a protocol for assessing irreversible inhibitors of TXNRD1. We describe four assays covering cellular TXNRD activity measurement, recombinant enzyme-based activity determination, differential scanning fluorimetry (DSF), and liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. This protocol will facilitate the screening and development of potential small-molecule inhibitors of TXNRD1.
硒蛋白硫氧还蛋白还原酶 1（TXNRD1）是一个很有前途的治疗靶点，已有报道称几种抑制剂能够抑制 TXNRD1 的活性。这些抑制剂有望应用于抗肿瘤药物等领域。本研究提供了一种评估 TXNRD1 不可逆抑制剂的方案。我们描述了四种测定方法，涵盖细胞 TXNRD 活性测定、基于重组酶的活性测定、差示扫描荧光法（DSF）和液相色谱-串联质谱法（LC-MS/MS）分析。本方案将有助于筛选和开发潜在的 TXNRD1 小分子抑制剂。
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