文献类型：期刊文献

英文题名：An Enzyme Kinetics-Based Laboratory Module Aimed at Introducing Undergraduates to High-Throughput Drug Screening

作者：He, Xiangli[1];Huang, Ying[2];Xu, Zhongyu[1];Liu, Xi[1];Xu, Zhaomin[1];Ma, Lei[1];Zhao, Yuzheng[1];Huang, Jin[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China;[2]Guangdong Inst Drug Control, Drug Inspect Technol, Guangzhou 510663, Peoples R China

年份：2023

卷号：100

期号：10

起止页码：3841

外文期刊名：JOURNAL OF CHEMICAL EDUCATION

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001061747800001)】；

基金：The authors thank the support from the Municipal-level Key Courses project from Shanghai Municipal Education Commission, the undergraduate education reform and construction project from East China University of Science and Technology, and the Science and Technology Project of Guangzhou (Grant No. 202102080640).

语种：英文

外文关键词：Upper-Division Undergraduate; Biochemistry; Enzyme Kinetics; High-Throughput Drug Screening; Hands-On Learning; Laboratory Education

摘要：Enzymes provide attractive targets for drug development. Quantitative analysis of enzyme reactions can lead to rational drug discovery. For undergraduates majoring in biochemistry or pharmacy and engaged in drug discovery-related work, it is essential to acquire a comprehensive understanding of enzyme kinetics, including experimental methods and the fundamental principles of drug screening. Being overexpressed in cancer, MTHFD2 is an emerging anticancer drug target. Herein, we used MTHFD2 to develop a high-throughput drug screening laboratory course based on enzyme kinetics for upper-division undergraduate students. The learning activities that were designed for students included Escherichia coli-based protein expression, protein purification, enzyme activity assay, setting up a high-throughput drug screening assay, and data analysis. The main purpose of this one-week laboratory education course is to provide students with a better understanding of enzyme kinetics, high-throughput drug screening and to help them grasp the relationship between enzyme kinetics and drug discovery. This hands-on course provides students an opportunity to learn how theoretical knowledge is applied in real practice.