Lu, Z;
Pham, TT;
Rajkumar, V;
Yu, Z;
Pedley, RB;
Årstad, E;
Maher, J;
(2018)
A Dual Reporter Iodinated Labeling Reagent for Cancer Positron Emission Tomography Imaging and Fluorescence-guided Surgery.
Journal of Medicinal Chemistry
, 61
(4)
pp. 1636-1645.
10.1021/acs.jmedchem.7b01746.
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Abstract
The combination of early diagnosis and complete surgical resection offers the greatest prospect of curative cancer treatment. An iodine-124/fluorescein-based dual-modality labeling reagent, 124I-Green, constitutes a generic tool for one-step installation of a positron emission tomography (PET) and a fluorescent reporter to any cancer-specific antibody. The resulting antibody conjugate would allow both cancer PET imaging and intraoperative fluorescence-guided surgery. 124I-Green was synthesized in excellent radiochemical yields of 92±5% (n=4) determined by HPLC with an improved one-pot three-component radioiodination reaction. The A5B7 carcinoembryonic antigen (CEA)-specific antibody was conjugated to 124I-Green. High tumour uptake of the dual-labeled A5B7 of 20.21±2.70, 13.31±0.73, and 10.64±1.86 %ID/g was observed in CEA-expressing SW1222 xenograft mouse model (n=3) at 24, 48, and 72 h post intravenous injection, respectively. The xenografts were clearly visualized by both PET/CT and ex vivo fluorescence imaging. These encouraging results warrant the further translational development of 124I-Green for cancer PET imaging and fluorescence-guided surgery.
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