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Thomas Poulsen

A Cyclopropene Electrophile that Targets Glutathione S-Transferase Omega-1 in Cells

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DOI

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).

Original languageEnglish
JournalAngewandte Chemie International Edition
Volume58
Issue34
Pages (from-to)11918-11922
Number of pages6
ISSN1433-7851
DOIs
Publication statusPublished - Jul 2019

    Research areas

  • chemical proteomics, bioorthogonal chemistry, cyclopropene, electrophiles, GSTO1 inhibition, DISCOVERY, REVEALS, POTENT, ANALOG

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