Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 18, Issue 31, Pages 6134-6139Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0ob01222j
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- Department of Radiology and Nuclear Medicine of Erasmus MC
- Laboratory of Experimental Surgical Oncology in the Department of Surgery at Erasmus MC
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We herein describe the development of a novel dual-modality optical/radio-imaging agent for general and site-specific labeling of biovectors through a 2-cyanobenzothiazole (CBT)/1,2-aminothiol click reaction. The CBT-based multifunctional single-attachment-point (MSAP) agent enables a single-step synthesis of various dual-modality probes characterized by rapid conjugation, high labeling yields, metabolically stable products and applicability to orthogonal two-step labeling of sensitive biomolecules. In addition, the two-step radiolabeling protocol and click reaction were optimized by using CBT scavengers to improve the reaction rate and molar activity of the imaging probes. Our methodology allows for a simple and efficient synthetic route to produce a variety of dual-modality imaging agents for preoperative surgical planning and intraoperative surgical guidance.
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