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Tumor cell membrane-coated continuous electrochemical sensor for GLUT1 inhibitor screening

摘要Glucose transporter 1(GLUT1)overexpression in tumor cells is a potential target for drug therapy,but few studies have reported screening GLUT1 inhibitors from natural or synthetic compounds.With cur-rent analysis techniques,it is difficult to accurately monitor the GLUT1 inhibitory effect of drug molecules in real-time.We developed a cell membrane-based glucose sensor(CMGS)that integrated a hydrogel electrode with tumor cell membranes to monitor GLUT1 transmembrane transport and screen for GLUT1 inhibitors in traditional Chinese medicines(TCMs).CMGS is compatible with cell membranes of various origins,including different types of tumors and cell lines with GLUT1 expression knocked down by small interfering RNA or small molecules.Based on CMGS continuous monitoring technique,we inves-tigated the glucose transport kinetics of cell membranes with varying levels of GLUT1 expression.We used CMGS to determine the GLUT1-inhibitory effects of drug monomers with similar structures from Scutellaria baicalensis and catechins families.Results were consistent with those of the cellular glucose uptake test and molecular-docking simulation.CMGS could accurately screen drug molecules in TCMs that inhibit GLUT1,providing a new strategy for studying transmembrane protein-receptor interactions.

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作者 Jiaqian Zhao [1] Yuqiao Liu [2] Ling Zhu [2] Junmin Li [2] Yanhui Liu [2] Jiarui Luo [2] Tian Xie [1] Dajing Chen [2] 学术成果认领
作者单位 School of Pharmacy,Hangzhou Normal University,Hangzhou,310000,China;Innovation Research Institute of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine,Shanghai,201203,China [1] School of Pharmacy,Hangzhou Normal University,Hangzhou,310000,China [2]
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DOI 10.1016/j.jpha.2023.04.015
发布时间 2023-08-07(万方平台首次上网日期,不代表论文的发表时间)
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药物分析学报(英文版)

药物分析学报(英文版)

2023年13卷6期

673-682页

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