English  |  正體中文  |  简体中文  |  Items with full text/Total items : 17744/20032 (89%)
Visitors : 7234305      Online Users : 342
RC Version 7.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
Scope Tips:
  • please add "double quotation mark" for query phrases to get precise results
  • please goto advance search for comprehansive author search
  • Adv. Search
    HomeLoginUploadHelpAboutAdminister Goto mobile version
    Please use this identifier to cite or link to this item: http://ir.cnu.edu.tw/handle/310902800/27685

    標題: An Activity-Based Near-Infrared Glucuronide Trapping Probe for Imaging beta-Glucuronidase Expression in Deep Tissues
    作者: Cheng, Ta-Chun
    Roffler, Steve R.
    Tzou, Shey-Cherng
    Chuang, Kuo-Hsiang
    Su, Yu-Cheng
    Chuang, Chih-Hung
    Kao, Chien-Han
    Chen, Chien-Shu
    Harn, I-Hong
    Liu, Kuan-Yi
    Cheng, Tian-Lu
    Leu, Yu-Ling
    貢獻者: 藥學系
    關鍵字: In-Vivo
    Reporter Gene
    Prodrug Monotherapy
    日期: 2012-02-15
    上傳時間: 2014-03-21 16:17:37 (UTC+8)
    出版者: Amer Chemical Soc
    摘要: beta-glucuronidase is an attractive reporter and prodrug-converting enzyme. The development of near-IR (NIR) probes for imaging of beta-glucuronidase activity would be ideal to allow estimation of reporter expression and for personalized glucuronide prodrug cancer therapy in preclinical studies. However, NIR glucuronide probes are not yet available. In this work, we developed two fluorescent probes for detection of beta-glucuronidase activity, one for the NIR range (containing IR-820 dye) and the other for the visible range [containing fluorescein isothiocyanate (FITC)], by utilizing a difluoromethylphenol-glucuronide moiety (TrapG) to trap the fluorochromes in the vicinity of the active enzyme. beta-glucuronidase-mediated hydrolysis of the glucuronyl bond of TrapG generates a highly reactive alkylating group that facilitates the attachment of the fluorochrome to nucleophilic moieties located near beta-glucuronidase-expressing sites. FITC-TrapG was selectively trapped on purified beta-glucuronidase or beta-glucuronidase-expressing CT26 cells (CT26/m beta G) but not on bovine serum albumin or non-beta-glucuronidase-expressing CT26 cells used as controls. beta-glucuronidase-activated FITC-TrapG did not interfere with beta-glucuronidase activity and could label bystander proteins near beta-glucuronidase. Both FITC-TrapG and NIR-TrapG specifically imaged subcutaneous CT26/m beta G tumors, but only NIR-TrapG could image CT26/m beta G tumors transplanted deep in the liver. Thus NIR-TrapG may provide a valuable tool for visualizing beta-glucuronidase activity in vivo.
    關聯: Journal of The American Chemical Society, 134(6), 3103-3110
    Appears in Collections:[藥學系(所)] 期刊論文

    Files in This Item:

    File Description SizeFormat

    All items in CNU IR are protected by copyright, with all rights reserved.

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - Feedback