The identification of new metallo-β-lactamase inhibitor leads from fragment-based screening

Peter Vella, Waleed M. Hussein, Eleanor W.W. Leung, Daniel Clayton, David L. Ollis, Nataša Mitić, Gerhard Schenk*, Ross P. McGeary

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    65 Citations (Scopus)

    Abstract

    The emergence of metallo-β-lactamases (MBLs) capable of hydrolysing a broad spectrum of β-lactam antibiotics is particularly concerning for the future treatment of bacterial infections. This work describes the discovery of lead compounds for the development of new inhibitors using a competitive colorimetric assay based on the chromogenic cephalosporin CENTA, and a 500 compound Maybridge™ library suitable for fragment-based screening. The interactions between identified inhibitory fragments and the active site of the MBL from Klebsiella pneumoniae and Pseudomonas aeruginosa were probed by in silico docking studies.

    Original languageEnglish
    Pages (from-to)3282-3285
    Number of pages4
    JournalBioorganic and Medicinal Chemistry Letters
    Volume21
    Issue number11
    DOIs
    Publication statusPublished - 1 Jun 2011

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