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Updated: Jan 22, 2026

Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
A Cyclopropene Electrophile that Targets Glutathione S-Transferase Omega-1 in Cells
Gustav J Wørmer1, Bente K Hansen1, Johan Palmfeldt2
1Department of Chemistry, Aarhus University, Langelandsgade 140, 8000, Aarhus C, Denmark.
Abstract:
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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