| 毛细管区带电泳测定D1蛋白酶的活性及其抑制剂先导化合物的筛选 |
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| 引用本文： | 陈腊月,李伟国,黄雪英,刘中来,刘艳丽,冯璐,廖宏珊,熊国梅,祁超.毛细管区带电泳测定D1蛋白酶的活性及其抑制剂先导化合物的筛选[J].分析化学,2011,39(11):1758-1761. |
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| 作者姓名： | 陈腊月 李伟国 黄雪英 刘中来 刘艳丽 冯璐 廖宏珊 熊国梅 祁超 |
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| 作者单位： | 华中师范大学生命科学学院遗传调控与整合生物学湖北省重点实验室;华中师范大学化学学院农药与化学生物学教育部重点实验室 |
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| 基金项目： | 国家自然科学基金(Nos.20702017,30670429);湖北省自然科学基金(Nos.2007ABA141,2010CDB01206,2009CDB234)资助 |
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| 摘 要： | 建立了毛细管区带电泳技术快速测定D1蛋白酶活性及其抑制剂先导化合物的筛选方法。实验选用未涂层熔融石英毛细管(43 cm 5mm)和磷酸盐缓冲溶液(50 mmol/L, pH 3.0)作为分离介质,运行电压18 kV,测定了D1蛋白酶的活性并对部分抑制剂先导化合物进行了筛选。结果表明, ITP26和ITP21两种异噁唑噻唑哌啶类先导化合物对蛋白酶活性具有抑制作用,抑制率分别为26%和13%。
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| 关 键 词： | D1蛋白酶 毛细管区带电泳 活性 先导化合物 |
| 收稿时间： | 7 March 2011 |
Determination of D1 Protease Activity and Screening for Lead Compounds of Inhibitor by Capillary Zone Electrophoresis |
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| La-Yue CHEN,Wei-Guo LI,Xue-Ying HUANG,Zhong-Lai LIU,Yan-Li LIU,Lu FENG,Hong-Shan LIAO,Guo-Mei XIONG,Chao QI.Determination of D1 Protease Activity and Screening for Lead Compounds of Inhibitor by Capillary Zone Electrophoresis[J].Chinese Journal of Analytical Chemistry,2011,39(11):1758-1761. |
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| Authors: | La-Yue CHEN Wei-Guo LI Xue-Ying HUANG Zhong-Lai LIU Yan-Li LIU Lu FENG Hong-Shan LIAO Guo-Mei XIONG Chao QI |
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| Institution: | aHubei Key Laboratory of Genetic Regulation & Integrative Biology, College of Life Science, Central China Normal University, Wuhan 430079, China;bKey Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China |
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| Abstract: | Capillary zone electrophoresis (CZE) with UV detection has been developed for the determination of D1 protease activity and screening for lead compounds of its inhibitor. Separation conditions of oligopeptides were optimized as phosphate buffer (50 mM, pH 3. 0) at a running voltage of 18 kV, with a capillary length of 43 cm × 75 μm (i.d). Hydrolysis activity assay of D1 protease and screening of lead compounds of its inhibitor were performed by CZE. In the study, two lead compounds, ITP 21 and ITP 26, showed inhibitory efficiency of 26% and 13%, respectively, while other compounds had no inhibitory effects on D1 protease activity. This method is simple, convenient and suitable for screening studies of the inhibitors of D1 protease. |
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| Keywords: | D1 protease Capillary zone electrophoresis Activity Lead compounds |
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