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An optimized ratiometric fluorescent probe for sensing human UDP-glucuronosyltransferase 1A1 and its biological applications
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
KeywordHuman Udp-glucuronosyltransferase 1a1 Ratiometric Fluorescent Probe Real Activity Biological Applications
Source PublicationBIOSENSORS & BIOELECTRONICS
2015-10-15
DOI10.1016/j.bios.2015.05.003
Volume72Pages:261-267
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
WOS SubjectBiophysics ; Biotechnology & Applied Microbiology ; Chemistry, Analytical ; Electrochemistry ; Nanoscience & Nanotechnology
WOS Research AreaBiophysics ; Biotechnology & Applied Microbiology ; Chemistry ; Electrochemistry ; Science & Technology - Other Topics
WOS KeywordLIVING CELLS ; INDUCED HYPERBILIRUBINEMIA ; BILIRUBIN GLUCURONIDATION ; UGT 1A1 ; DRUG ; CANCER ; PHARMACOGENOMICS ; INHIBITION ; METABOLISM ; NILOTINIB
AbstractThis 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.
Language英语
WOS IDWOS:000356734000038
Citation statistics
Cited Times:25[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/146344
Collection中国科学院大连化学物理研究所
Affiliation1.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
GB/T 7714
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.
APA Lv, Xia.,Ge, Guang-Bo.,Feng, Lei.,Troberg, Johanna.,Hu, Liang-Hai.,...&Yang, Ling.(2015).An optimized ratiometric fluorescent probe for sensing human UDP-glucuronosyltransferase 1A1 and its biological applications.BIOSENSORS & BIOELECTRONICS,72,261-267.
MLA Lv, Xia,et al."An optimized ratiometric fluorescent probe for sensing human UDP-glucuronosyltransferase 1A1 and its biological applications".BIOSENSORS & BIOELECTRONICS 72(2015):261-267.
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