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Degrasyn exhibits antibiotic activity against multi-resistant Staphylococcus aureus by modifying several essential cysteines

ABSTRACT: In this dataset, we investigate the targets of degrasyn in the methicillin-sensitive S. aureus strain NCTC 8325. This includes data on enrichment studies and competition studies with conventional ABPP using a degrasyn-derived probe, competition studies with residue-specific proteomics using the isoDTB-ABPP method and global analysis of protein expression levels in response to degrasyn treatment.

INSTRUMENT(S): Orbitrap Fusion, Q Exactive

ORGANISM(S): Staphylococcus Aureus

SUBMITTER: Stephan M. Hacker

LAB HEAD: Stephan A. Sieber

PROVIDER: PXD016413 | Pride | 2020-04-14

REPOSITORIES: Pride

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Degrasyn exhibits antibiotic activity against multi-resistant Staphylococcus aureus by modifying several essential cysteines.

Lee Kyu Myung KM Le Philipp P Sieber Stephan A SA Hacker Stephan M SM

Chemical communications (Cambridge, England) 20200301 19

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. ...[more]

PMID: 32039420

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