Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 61, Issue 50, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202213495
Keywords
F-19 MRI; Biosensors; Fluorescence Imaging; Hypoxia; Nitroreductase
Categories
Funding
- Key Technology Research and Development Program [2018YFA0704000]
- Tencent Foundation through the XPLORER PRIZE
- National Natural Science Foundation of China [91859206, 21874150, U21A20392, 82127802, 21921004]
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FCy7-NO2, a novel dual-mode NIR fluorescence and F-19 MRI agent, is proposed for imaging tumor hypoxia, showing rapid monitoring of nitroreductase in tumors and sensitive detection over a broad concentration range without limits to imaging depth by integrating two complementary imaging technologies.
Nitroreductase (NTR) is an important biomarker widely used to evaluate the degree of tumor hypoxia. Although a few optical methods have been reported for detecting nitroreductase at low concentration ranges, an effective strategy for nitroreductase monitoring in vivo without limits to the imaging depth is still lacking. Herein, a novel dual-mode NIR fluorescence and F-19 MRI agent, FCy7-NO2, is proposed for imaging tumor hypoxia. We show that FCy7-NO2 serves as not only a rapid NIR fluorescence enhanced probe for monitoring and bioimaging of nitroreductase in tumors, but also a novel F-19 MR chemical shift-sensitive contrast agent for selectively detecting nitroreductase catalyzed reduction. Notably, integrating two complementary imaging technologies into FCy7-NO2 enables sensitive detection of nitroreductase in a broad concentration range without tissue-depth limit. In general, this agent has a remarkable response to nitroreductase, which provides a promising method for understanding tumor evolution and its physiological role in the hypoxic microenvironment.
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