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Irreversible inhibition of the bacterial cysteine protease-transpeptidase sortase (SrtA) by substrate-derived affinity labels



Irreversible inhibition of the bacterial cysteine protease-transpeptidase sortase (SrtA) by substrate-derived affinity labels



Biochemical Journal 366(Pt 3): 953-958



We report on the first synthesis, kinetic evaluation and application of novel substrate-derived inhibitors against the Staphylococcus aureus cysteine protease-transpeptidase, sortase (staphylococcal surface protein sorting A, SrtA). The peptidyl-diazomethane and peptidyl-chloromethane analogues, Cbz (benzyloxycarbonyl)-Leu-Pro-Ala-Thr-CHN2 (I) and Cbz-Leu-Pro-Ala-Thr-CH2Cl (II) respectively were found to act as time-dependent irreversible inhibitors of recombinant sortase (SrtADELTAN).

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Accession: 010885743

Download citation: RISBibTeXText

PMID: 12069686

DOI: 10.1042/BJ20020602



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