Journal
ANALYTICAL CHEMISTRY
Volume 92, Issue 17, Pages 11627-11634Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.analchem.0c01253
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Funding
- National Natural Science Foundation of China [81972906]
- Natural Science Foundation of Jiangsu Province [BK20181128]
- Project 333 of Jiangsu Province [LGY2018086]
- Key Youth Medical Talent Project of Jiangsu Province [QNRC2016626, QNRC2016629]
- Precision Medical Project of Wuxi Commission of Health and Family Planning [J201806]
- Major Scientific Research Project of Wuxi Commission of Health [Z201913]
- Innovation Capacity Development Plan of Jiangsu Province [BM2018023]
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Overexpression of legumain is closely associated with tumor proliferation, invasion, and metastasis. Because of its intrinsic properties, such as high sensitivity and resolution, positron emission tomography (PET) has become an effective imaging technique for early diagnosis, treatment response prediction, and monitoring. Herein, two legumain-targeting radiofluorinated smart probes (F-18-2 and F-18-3) as well as a control probe (F-18-1) were specifically designed for PET imaging of legumain activity in tumors.F-18-1, F-18-2, and F-18-3 were obtained with high radiochemical yield (RCY > 60%) and radiochemical purity (RCP > 99%) using a convenient one-step F-18-labeling method. The probes F-18-2 and F-18-3 exhibited high response to legumain activity and reductive environment and revealed comparable uptake in HCT116 cells (4.22% +/- 0.14% and 4.64% +/- 0.32% for F-18-2 and F-18-3, respectively; 8.46% +/- 0.33% and 9.05% +/- 0.24% for co-treatment of F-18-2 + 2 and F-18-3 + 3 at 1 h), while the control probe F-18-1 showed no response. PET imaging of tumor-bearing mice showed that the co-injection strategy (F-18-2 + 2 and F-18-3 + 3) resulted in higher tumor uptake (3.57% +/- 0.37% and 3.72% +/- 0.19% ID/g at 10 min, respectively) than the single injection strategy (2.59% +/- 0.19% and 2.60% +/- 0.46% ID/g for F-18-2 and 18 F-3, respectively). In addition, introduction of the trimeric histidine-glutamate (HEHEHE) tag to F-18-3 reduced the liver uptake by almost two-fold without any noticeable effect on the tumor uptake. All the results indicate that F-18-3 holds great potential applications in clinics for sensitive and specific PET imaging of legumain activity in tumors.
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