Endoplasmic Reticulum-Targeting Near-Infrared Fluorescent Probe for CYP2J2 Activity and Its Imaging Application in Endoplasmic Reticulum Stress and Tumor
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Published on: May 7, 2013
Xiangge Tian1,2,3, Tao Liu4, Mingyue Zhu2
1Department of Pharmacy, Peking University Shenzhen Hospital, Shenzhen 518036, China.
Abstract:
CYP2J2 as an endoplasmic reticulum (ER)-expressed vital cytochrome P450 isoform participates in the metabolism of endogenous polyunsaturated fatty acids. Its abnormal expression and function are closely related to the progress of cancer and cardiovascular diseases. Herein, an ER-targeting near-infrared (NIR) fluorescent probe ER-BnXPI was developed for monitoring CYP2J2 activity, which possessed a high selectivity and sensitivity toward CYP2J2 among various CYP450 isoforms and exhibited excellent subcellular localization for ER. Then, the CYP2J2 variation behavior under the ER stress model was imaged by ER-BnXPI in living cells and successfully used for the in vivo imaging in different tumors that well distinguished tumor tissues from para-cancerous tissues. All these findings fully demonstrated that ER-BnXPI could be used as a promising tool for exploring the physiological function of CYP2J2 and provided some novel approach for the diagnosis and therapy of CYP2J2-related vascular inflammation and cancer.
Insights
A new near-infrared fluorescent probe, ER-BnXPI, effectively monitors endoplasmic reticulum (ER) enzyme CYP2J2 activity. This tool aids in understanding ER stress and diagnosing related cancers and cardiovascular diseases.
Area of Science:
- Biochemistry
- Molecular Biology
- Medical Imaging
Background:
- Cytochrome P450 2J2 (CYP2J2) is crucial for metabolizing polyunsaturated fatty acids.
- Abnormal CYP2J2 expression is linked to cancer and cardiovascular disease progression.
- Targeting endoplasmic reticulum (ER) enzyme activity is vital for disease monitoring.
Purpose of the Study:
- To develop a selective and sensitive probe for monitoring CYP2J2 activity in the ER.
- To visualize CYP2J2 activity changes under ER stress conditions.
- To assess the probe's utility in diagnosing CYP2J2-related diseases.
Main Methods:
- Development of an ER-targeting, near-infrared (NIR) fluorescent probe, ER-BnXPI.
- Testing probe selectivity and sensitivity against various CYP450 isoforms.
- Imaging CYP2J2 activity in living cells under ER stress models.
- In vivo imaging of ER-BnXPI in tumor models.
Main Results:
- ER-BnXPI demonstrated high selectivity and sensitivity for CYP2J2.
- The probe showed excellent endoplasmic reticulum localization.
- CYP2J2 activity variations were successfully imaged in living cells and in vivo tumors.
- Tumor tissues were clearly distinguished from para-cancerous tissues.
Conclusions:
- ER-BnXPI is a promising tool for studying CYP2J2 physiological functions.
- The probe offers a novel approach for diagnosing CYP2J2-related vascular inflammation and cancer.
- ER-BnXPI facilitates exploration of ER stress mechanisms and disease pathology.
