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Published on: September 14, 2018
An Orthogonally Functionalizable Tetrazine Building Block for Dual-Conjugated Bioorthogonal Probes
Bing-Feng Wang1, Ke Chen1,2, Xirui Liu1
1Department of Radiology, Huaxi MR Research Center (HMRRC), Institute of Radiology and Medical Imaging, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, China.
Abstract:
The development of multifunctional bioorthogonal tools is essential for expanding their utility in biomedical research. Here, we report a gram-scale accessible building block, 3-(mesyloxyethyl)-6-(diethylphosphonomethyl)-tetrazine, featuring two orthogonal reactive handles. This scaffold enables the modular construction of a series of dual-conjugated tetrazine probes with versatile functionalities. Remarkably, the dual-conjugated architecture was found to induce bathochromic emission in the resulting bioorthogonal adducts, thereby facilitating new fluorophores in situ formation and offering a promising platform for the design of theranostic agents.
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