Development of ¹⁸F-Labeled Bispyridyl Tetrazines for In Vivo Pretargeted PET Imaging.

ABSTRACT: Pretargeted PET imaging is an emerging and fast-developing method to monitor immuno-oncology strategies. Currently, tetrazine ligation is considered the most promising bioorthogonal reaction for pretargeting in vivo. Recently, we have developed a method to ¹⁸F-label ultrareactive tetrazines by copper-mediated fluorinations. However, bispyridyl tetrazines-one of the most promising structures for in vivo pretargeted applications-were inaccessible using this strategy. We believed that our successful efforts to ¹⁸F-label H-tetrazines using low basic labeling conditions could also be used to label bispyridyl tetrazines via aliphatic nucleophilic substitution. Here, we report the first direct ¹⁸F-labeling of bispyridyl tetrazines, their optimization for in vivo u

SUBMITTER: Garcia-Vazquez R 

PROVIDER: S-EPMC8879724 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature