Tetravalent Pseudomonas aeruginosa Adhesion Lectin LecA Inhibitor for Enhanced Biofilm Inhibition

A potent divalent ligand of the Pseudomonas aeruginosa adhesion lectin LecA was elaborated into a tetravalent version. A polyethylene glycol (PEG) spacer was introduced to link two divalent galactosides. Each of the two divalent ligands contained a rigid spacer with a central phenyl group that is br...

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Bibliographic Details
Published in:Helvetica chimica acta 2019-03, Vol.102 (3), p.n/a
Main Authors: Yu, Guangyun, Thies‐Weesie, Dominique M. E., Pieters, Roland J.
Format: Article
Language:English
Subjects:
Adhesion
analytical methods
analytical ultracentrifugation
biofilm inhibition
Biofilms
Galactosides
Inhibition
Inhibitors
ITC
Ligands
multivalent carbohydrates
Polyethylene glycol
Pseudomonas aeruginosa
Sugar
Ultracentrifugation
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Summary:A potent divalent ligand of the Pseudomonas aeruginosa adhesion lectin LecA was elaborated into a tetravalent version. A polyethylene glycol (PEG) spacer was introduced to link two divalent galactosides. Each of the two divalent ligands contained a rigid spacer with a central phenyl group that is bridged by the PEG moiety. The resulting tetravalent ligand was found to bind LecA in the nanomolar range involving all of its sugar (sub)ligands. Analytical ultracentrifugation studies clearly showed that the tetravalent ligand was capable of aggregation the LecA tetramers in contrast to the divalent ligands. The aggregator behavior was found to be of importance in P. aeruginosa biofilm formation inhibition. Despite the weaker affinity it was a considerably better biofilm inhibitor with half inhibitory values around the 28 micromolar range.
ISSN:0018-019X
1522-2675
DOI:10.1002/hlca.201900014