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题名: An optimized ratiometric fluorescent probe for sensing human UDP-glucuronosyltransferase 1A1 and its biological applications
作者: Lv, Xia1;  Ge, Guang-Bo1, 2;  Feng, Lei2;  Troberg, Johanna3;  Hu, Liang-Hai4;  Hou, Jie;  Cheng, Hai-Ling5;  Wang, Ping1;  Liu, Zhao-Ming1;  Finel, Moshe3;  Cui, Jing-Nan2;  Yang, Ling1
关键词: Human UDP-glucuronosyltransferase 1A1 ;  Ratiometric fluorescent probe ;  Real activity ;  Biological applications
刊名: BIOSENSORS & BIOELECTRONICS
发表日期: 2015-10-15
DOI: 10.1016/j.bios.2015.05.003
卷: 72, 页:261-267
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine ;  Physical Sciences
类目[WOS]: Biophysics ;  Biotechnology & Applied Microbiology ;  Chemistry, Analytical ;  Electrochemistry ;  Nanoscience & Nanotechnology
研究领域[WOS]: Biophysics ;  Biotechnology & Applied Microbiology ;  Chemistry ;  Electrochemistry ;  Science & Technology - Other Topics
英文摘要: This study aimed to develop a practical ratiometric fluorescent probe for highly selective and sensitive detection of human UDP-glucuronosyltransferase 1A1 (UGT1A1), one of the most important phase II enzymes. 4-Hydroxy-1,8-naphthalimide (HN) was selected as the fluorophore for this study because it possesses intramolecular charge transfer (ICT) feature and displays outstanding optical properties. A series of N-substituted derivatives with various hydrophobic, acidic and basic groups were designed and synthesized to evaluate the selectivity of HN derivatives toward UGT1A1. Our results demonstrated that the introduction of an acidic group to HN could significantly improve the selectivity of UGT1A1. Among the synthesized fluorescent probes, NCHN (N-3-carboxy propy1-4-hydroxy-1,8-naphthalimide) displayed the best combination of selectivity, sensitivity and ratiometric fluorescence response following UGT1A1-catalyzed glucuronidation. UGT1A1-catalyzed NCHN-4-O-glucuronidation generated a single fluorescent product with a high quantum yield (Phi=0.688) and brought remarkable changes in both color and fluorescence in comparison with the parental substrate. The newly developed probe has been successfully applied for sensitive measurements of UGT1A1 activities in human liver preparations, as well as for rapid screening of UGT1A1 modulators, using variable enzyme sources. Furthermore, its potential applications for live imaging of endogenous UGT1A1in cells have also been demonstrated. (C) 2015 Elsevier B.V. All rights reserved.
关键词[WOS]: LIVING CELLS ;  INDUCED HYPERBILIRUBINEMIA ;  BILIRUBIN GLUCURONIDATION ;  UGT 1A1 ;  DRUG ;  CANCER ;  PHARMACOGENOMICS ;  INHIBITION ;  METABOLISM ;  NILOTINIB
语种: 英语
WOS记录号: WOS:000356734000038
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/146344
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
2.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China
3.Univ Helsinki, Fac Pharm, Div Pharmaceut Chem & Technol, Helsinki, Finland
4.Jilin Univ, Coll Life Sci, Changchun 130023, Peoples R China
5.Dalian Med Univ, Dalian 116044, Peoples R China

Recommended Citation:
Lv, Xia,Ge, Guang-Bo,Feng, Lei,et al. An optimized ratiometric fluorescent probe for sensing human UDP-glucuronosyltransferase 1A1 and its biological applications[J]. BIOSENSORS & BIOELECTRONICS,2015,72:261-267.
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