Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 34, Pages 11918-11922Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201907520
Keywords
chemical proteomics; bioorthogonal chemistry; cyclopropene; electrophiles; GSTO1 inhibition
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Funding
- Carlsberg foundation [CF17-0800]
- Independent Research Fund Denmark (Sapere Aude 2 grant) [6110-00600A]
- Novo Nordisk Foundation [NNF19OC0054782]
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Cyclopropenes are an important new addition to the portfolio of functional groups that can be used for bioorthogonal couplings. The inert nature of these highly strained compounds in complex biological systems is almost counterintuitive given their established electrophilic properties in organic synthesis. Here we provide the first demonstration of a cyclopropene that is capable of direct conjugation to protein targets in cells and show that this compound preferentially alkylates the active site cysteine of glutathione S-transferase omega-1 (GSTO1).
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