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Issue 31, 2020
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A novel clickable MSAP agent for dual fluorescence/nuclear labeling of biovectors

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Abstract

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.

Graphical abstract: A novel clickable MSAP agent for dual fluorescence/nuclear labeling of biovectors

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Supplementary files

Article information


Submitted
14 Jun 2020
Accepted
10 Jul 2020
First published
10 Jul 2020

Org. Biomol. Chem., 2020,18, 6134-6139
Article type
Paper

A novel clickable MSAP agent for dual fluorescence/nuclear labeling of biovectors

K. Chen, J. Nieuwenhuizen, M. Handula and Y. Seimbille, Org. Biomol. Chem., 2020, 18, 6134
DOI: 10.1039/D0OB01222J

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