文章摘要
王婷 阮林高 戈梅 钱秀萍.一种利用荧光标记检测氨肽酶N抑制剂与肿瘤细胞结合的方法[J].,2014,14(4):634-638
一种利用荧光标记检测氨肽酶N抑制剂与肿瘤细胞结合的方法
A method for Detecting the Binding Activities of Aminopeptidase NInhibitors to Tumor Cell by Fluorescein
  
DOI:
中文关键词: 氨肽酶N 抑制剂  LYRM03  Bestatin  异硫氰酸荧光素
英文关键词: Aminopeptidase N inhibitors  LYRM03  Bestatin  Fluorescein isothiocyanate(FITC)
基金项目:国家重大新药创制专项(2010zx09401-403)
作者单位
王婷 阮林高 戈梅 钱秀萍 上海交通大学药学院
上海来益生物药物研发中心 
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中文摘要:
      目的:建立利用荧光标记法检测氨肽酶抑制剂和肿瘤细胞结合的方法。方法:以异硫氰酸荧光素(FITC)标记氨肽酶N抑制 剂LYRM03 和Bestatin,制备荧光探针FITC-LYRM03、FITC-Bestatin,应用荧光显微成像观察和流式细胞仪检测标记化合物 FITC-LYRM03、FITC-Bestatin对肿瘤细胞的结合与氨肽酶N 抑制活性的相关性。结果:化合物LYRM03 和Bestatin 具有肿瘤细 胞的氨肽酶N抑制活性,荧光标记化合物FITC-LYRM03、FITC-Bestatin 能与肿瘤细胞有不同程度的结合。结论:标记化合物 FITC-LYRM03、FITC-Bestatin和肿瘤细胞的结合与对肿瘤细胞的氨肽酶N抑制活性相一致。
英文摘要:
      Objective:To build a fluorescein labeling method to detect the bingding of aminopeptidase N inhibitors with tumor cells.Methods:AminopeptidaseN inhibitors LYRM03 and Bestatin were labeled with fluorescein isothiocyanate (FITC), and fluorescein -labeled compounds of FITC-LYRM03 and FITC-Bestatin were purified. The relationship between binding activities to tumor cells and inhibitory activities of aminopeptidase N inhibitors was detected by using fluorescence microscope and flow cytometer. Results:Compounds of LYRM03 and Bestatin had inhibitory activities to aminopeptidase N of tumor cells. Fluorescein-labeled FITC-LYRM03 and FITC-Bestatin had different binding activities to tumor cells.Conclusion:There was consistency between binding activities of tumor cells and inhibitory activities of aminopeptidase N inhibitors.
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