Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

An electronic equilibrium strategy to drive the design of reversible fluorescent probes for sulfur dioxide and formaldehyde.

Chemical science·2026

Same author

Enzyme-Activatable Fluorogenic Probes: Design Strategies, Biomedical Applications, and Future Perspectives.

Journal of the American Chemical Society·2026

Same author

Photocaged Fluorogenic Glycoprobes for Light-Activatable Sensing and Imaging of Galactosidase Activities in Live Cells.

ACS sensors·2026

Same author

Targeted degradation of hepatic KEAP1 mitigates drug-induced liver injury via dual boosting NRF2 and PGAM5 signaling.

Redox biology·2026

Same author

Synthesis of divalent galactosyl and fucosyl spiropyran derivatives for the targeted inhibition of bacterial biofilms.

Chemical communications (Cambridge, England)·2026

Same author

Large-area two-dimensional MoO<sub>3</sub> as a high-κ dielectric for van der Waals integration.

Nature communications·2026

Search research articles

Related Experiment Video

Updated: Sep 20, 2025

Non-invasive In Vivo Fluorescence Optical Imaging of Inflammatory MMP Activity Using an Activatable Fluorescent Imaging Agent

Non-invasive In Vivo Fluorescence Optical Imaging of Inflammatory MMP Activity Using an Activatable Fluorescent Imaging Agent

Published on: May 8, 2017

An optimized CYP3A4-activatable fluorogenic sensor for in situ functional imaging and multi-dimensional inhibitor

Feng Zhang¹, Yufan Fan¹, Mei Luo¹

¹State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shanghai Frontiers Science Center of TCM Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine Shanghai 201203 China geguangbo@shutcm.edu.cn.

Chemical Science

|May 26, 2025

Summary

Researchers developed a novel fluorogenic sensor, N-cyclopropylmethyl-1,8-naphthalimide (NCN), for precisely measuring Cytochrome P450 3A4 (CYP3A4) activity. This tool enables in situ imaging and inhibitor assessment in living systems without P-gp interference.

More Related Videos

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog

Published on: November 5, 2014

Open Source High Content Analysis Utilizing Automated Fluorescence Lifetime Imaging Microscopy

Open Source High Content Analysis Utilizing Automated Fluorescence Lifetime Imaging Microscopy

Published on: January 18, 2017

Related Experiment Videos

Last Updated: Sep 20, 2025

Non-invasive In Vivo Fluorescence Optical Imaging of Inflammatory MMP Activity Using an Activatable Fluorescent Imaging Agent

Non-invasive In Vivo Fluorescence Optical Imaging of Inflammatory MMP Activity Using an Activatable Fluorescent Imaging Agent

Published on: May 8, 2017

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog

Published on: November 5, 2014

Open Source High Content Analysis Utilizing Automated Fluorescence Lifetime Imaging Microscopy

Open Source High Content Analysis Utilizing Automated Fluorescence Lifetime Imaging Microscopy

Published on: January 18, 2017

Area of Science:

Biochemistry
Pharmacology
Chemical Biology

Background:

Cytochrome P450 3A4 (CYP3A4) is a critical drug-metabolizing enzyme.
Accurate tools are needed to monitor CYP3A4 activity in complex biological systems.
Understanding CYP3A4 modulation is vital for drug development and patient safety.

Purpose of the Study:

To develop an optimized CYP3A4-activatable fluorogenic sensor for in situ detection.
To create a tool that avoids interference from P-glycoprotein (P-gp).
To enable precise assessment of CYP3A4 inhibitors across various biological systems.

Main Methods:

Integrated strategy involving computer-aided design, drug-likeness filtering, and biochemical assays.
Screening of 1,8-naphthalimide derivatives to identify an optimal CYP3A4 substrate.
Evaluation of the sensor's specificity, sensitivity, cell permeability, bio-safety, and P-gp interaction.

Main Results:

Identified N-cyclopropylmethyl-1,8-naphthalimide (NCN) as a highly specific and sensitive CYP3A4 fluorogenic substrate.
NCN and its metabolite HNCN are non-substrates of P-gp, facilitating in situ imaging.
NCN demonstrated oral bioavailability, enabling multi-dimensional assessment of CYP3A4 inhibitors.

Conclusions:

NCN is a practical and reliable tool for in situ CYP3A4 activity imaging.
The developed sensor enables precise assessment of CYP3A4 inhibitors in vitro, ex vivo, and in vivo.
This work presents a rational engineering strategy for developing isoform-specific, orally bioavailable CYP3A4 substrates.