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Updated: Dec 28, 2025

Improved Enzyme Protection Assay to Study Staphylococcus aureus Internalization and Intracellular Efficacy of Antimicrobial Compounds
Published on: September 8, 2021
Degrasyn exhibits antibiotic activity against multi-resistant Staphylococcus aureus by modifying several essential
Kyu Myung Lee1, Philipp Le1, Stephan A Sieber1
1Center for Integrated Protein Science, Department of Chemistry and Chair of Organic Chemistry II, Technische Universität München, Garching bei München, Germany. stephan.sieber@tum.de.
None:
Degrasyn inhibits deubiquitination enzymes and has anti-cancer activity. We here show that it also exhibits antimicrobial activity against multi-resistant Staphylococcus aureus. Structure activity relationship studies demonstrate an important role of the electrophilic α-cyanoacrylamide moiety as a Michael acceptor. A suite of chemical proteomic techniques unraveled binding of this moiety to various cysteine residues of essential proteins in a reversibly covalent manner.
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