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Issue 31, 2013
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Antagonism of a zinc metalloprotease using a unique metal-chelating scaffold: tropolones as inhibitors of P. aeruginosa elastase

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Abstract

Tropolone emerged from the screening of a chelator fragment library (CFL) as an inhibitor of the Zn2+-dependent virulence factor, Pseudomonas aeruginosa elastase (LasB). Based on this initial hit, a series of substituted tropolone-based LasB inhibitors was prepared, and a compound displaying potent activity in vitro and in a bacterial swarming assay was identified. Importantly, this inhibitor was found to be specific for LasB over other metalloenzymes, validating the usage of tropolone as a viable scaffold for identifying first-in-class LasB inhibitors.

Graphical abstract: Antagonism of a zinc metalloprotease using a unique metal-chelating scaffold: tropolones as inhibitors of P. aeruginosa elastase

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Publication details

The article was received on 13 Feb 2013, accepted on 05 Mar 2013 and first published on 06 Mar 2013


Article type: Communication
DOI: 10.1039/C3CC41191E
Citation: Chem. Commun., 2013,49, 3197-3199
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    Antagonism of a zinc metalloprotease using a unique metal-chelating scaffold: tropolones as inhibitors of P. aeruginosa elastase

    J. L. Fullagar, A. L. Garner, A. K. Struss, J. A. Day, D. P. Martin, J. Yu, X. Cai, K. D. Janda and S. M. Cohen, Chem. Commun., 2013, 49, 3197
    DOI: 10.1039/C3CC41191E

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