Fluorescent probes for the detection and imaging of Cytochrome P450

Lei Feng, Jing Ning, Xiangge Tian, Chao Wang, Zhenlong Yu, Xiaokui Huo, Tian Xie, Baojing Zhang, Tony D. James, Xiaochi Ma

Research output: Contribution to journalReview articlepeer-review

25 Citations (SciVal)


Cytochrome P450 (CYP) enzymes are haem-containing proteins which are mainly involved in the oxidative metabolism of various chemicals. CYP enzymes can be affected by co-administrated drugs, environmental factors, disease states and genetic polymorphism, leading to differing degrees of individual variability of CYP activity which can induce the adverse effect of drugs or result in the failure of a drug therapy with varying severity. In this arena, fluorescent probes can serve as useful molecular tools to selectively detect CYP activity, facilitated by their intrinsic sensitivity and capacity for rapid, real-time and in situ monitoring as well as high-throughput screening. Therefore, the design of enzymatic activity reporters serving as the CYP subtype-specific probes, has stimulated widespread interest. This review covers the design principles for probes and systemically summarizes recent advances in the development of fluorescent probes for CYP isoforms including CYP1A, CYP1A1, CYP2C9, CYP2D6, CYP2J2, CYP3A, CYP3A4, CYP3A7, CYP4A11, CYP4F12 and CYP4F3B, and also probes for detecting the reduction ability of CYP, then categorizes these molecular tools according to the detection strategy or interaction models for the key CYP isoforms, such as dealkylation, hydroxylation or reduction reactions. In addition, challenges and future perspectives in the development of selective and sensitive fluorescent probes of CYP are discussed.

Original languageEnglish
Article number213740
JournalCoordination Chemistry Reviews
Early online date19 Mar 2021
Publication statusPublished - 15 Jun 2021

Bibliographical note

Funding Information:
The authors thank the National Natural Science Foundation of China (81930112, 82004211, 81730108 and 81503152), National Key Research and Development Program of China (No. 2018YFC1705900), Liaoning Provincial Key R&D Program (2019JH2/10300022), Distinguished professor of Liaoning Province, Dalian Science and Technology Leading Talents Project (2019RD15), State Key Laboratory of Fine Chemicals (KF1912) Scientific research fund of Hangzhou Normal University, for financial support. T.D.J. wishes to thank the Royal Society for a Wolfson Research Merit Award and the Open Research Fund of the School of Chemistry and Chemical Engineering, Henan Normal University for support (2020ZD01).

Publisher Copyright:
© 2020 Elsevier B.V.

Copyright 2021 Elsevier B.V., All rights reserved.


  • Cytochrome P450
  • Enzyme detection
  • Fluorescence bioimaging
  • Fluorescent probes

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Inorganic Chemistry
  • Materials Chemistry


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