期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 49, 页码 15612-15616出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201708790
关键词
bioorthogonal reactions; chemical biology; cleavage reactions; click chemistry; mesoionic compounds
资金
- French National Research Agency [ANR-14-CE06-0004]
We report the discovery of a new bioorthogonal click-and-release reaction involving iminosydnones and strained alkynes. This transformation leads to two products resulting from the ligation and fragmentation of iminosydnones under physiological conditions. Optimized iminosydnones were successfully used to design innovative cleavable linkers for protein modification, thus opening up new areas in the fields of drug release and target-fishing applications. This click-and-release technology offers the possibility of exchanging tags on proteins for functionalized cyclooctynes under mild and bioorthogonal conditions.
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