Fluorescent probes for bioactive detection and imaging of phase II metabolic enzymes

Lei Feng, Jing Ning, Xiangge Tian, Chao Wang, Liyuan Zhang, Xiaochi Ma, Tony D. James

Research output: Contribution to journalReview articlepeer-review

39 Citations (SciVal)

Abstract

Numerous enzymes with diverse structures and functions are distributed in nature, and their expressions and functions are easily influenced by genetic and environmental factors, resulting in their presence in different tissues, individuals and species. The metabolic enzymes are responsible for modification of functional groups (classified as phase I reactions) or conjugation with endogenous substituents (classified as phase II reactions) in the organism. Fluorescent probes are key tools in the characterization of metabolic enzymes, used in drug discovery, evaluation of drug-drug interactions, clinical diagnosis and treatment etc. Therefore, the use of fluorescent probes in the accurate and rapid detection of phase II metabolic enzymes and related applications are summarized in this review. In particular, the following enzymes will be covered: UGT (Uridine-diphosphate glucuronosyltransferase), COMT (Catechol-O-methyltransferase), NAT (N-acetyltransferase), GT (Glucosyltransferase), GST (Glutathione S-transferase), SULT (Sulfotransferase) and some other phase II metabolic enzymes. Their applications to biological imaging and high-throughput inhibitor screening are discussed in detail. In addition, future directions in the design and development of small molecular fluorescent probes for phase II enzymes are discussed in the final section.

Original languageEnglish
Article number213026
JournalCoordination Chemistry Reviews
Volume399
Early online date29 Aug 2019
DOIs
Publication statusPublished - 15 Nov 2019

Funding

The authors thank the National Natural Science Foundation of China ( 81930112 , 81622047 , 81503201 and 81874301 ), the Fundamental Research Funds for Central University (Grant: DLUT15QY43 ), National Key R&D Program of China ( 2018YFC1705900 ), Distinguished Professor of Liaoning Province program, State Key Laboratory of Fine Chemicals ( KF1803 ), Open Research Fund of the State Key Laboratory of Cognitive Neuroscience and Learning ( CNLZD1801 ) for financial support. T.D.J. wishes to thank the Royal Society for a Wolfson Research Merit Award .

Keywords

  • Enzyme detection
  • Fluorescence bioimaging
  • Fluorescent probes
  • High-throughput inhibitor screening
  • Phase II metabolic enzymes

ASJC Scopus subject areas

  • General Chemistry
  • Physical and Theoretical Chemistry
  • Inorganic Chemistry
  • Materials Chemistry

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