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A simple screen for murein transglycosylase inhibitors

Lookup NU author(s): Professor Waldemar Vollmer

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Abstract

A simple assay for detection of compounds that bind to the active site in the transglycosylation domain of the essential bifunctional transglycosylase and transpeptidase penicillin-binding proteins (PBPs) is reported. The method is based on a competition with the specific transglycosylase inhibitor moenomycin. With moenomycin coupled to Affi-Gel beads, a simple filtration procedure allows the amount of labeled PBPs that bind to moenomycin beads in the presence of test substances to be determined. The PBPs can easily be labeled by the covalent binding of penicillin derivatives. Crude membrane extracts can be used as a source for the PBPs, and different kinds of labels for the penicillin-PBP complexes can be used. The assay can be adapted to high-throughput screens.

Publication metadata

Author(s): Vollmer W, Höltje J-V

Publication type: Article

Publication status: Published

Journal: Antimicrobial Agents and Chemotherapy

Year: 2000

Volume: 44

Issue: 5

Pages: 1181-1185

ISSN (print): 0066-4804

ISSN (electronic): 1098-6596

Publisher: American Society for Microbiology

URL: http://dx.doi.org/10.1128/AAC.44.5.1181-1185.2000

DOI: 10.1128/AAC.44.5.1181-1185.2000

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