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.

doi.org/10.1039/d0ob01222j, hdl.handle.net/1765/129658
Organic & biomolecular chemistry
Department of Radiology

Chen, K.-T. (Kuo-Ting), Nieuwenhuizen, J. (Jim), Handula, M. (Maryana), & Seimbille, Y. (Yann). (2020). A novel clickable MSAP agent for dual fluorescence/nuclear labeling of biovectors. Organic & biomolecular chemistry, 18(31), 6134–6139. doi:10.1039/d0ob01222j