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A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d-galactose pentaacetate.
Zahorska, Eva Kuhaudomlarp, Sakonwan Minervini, Saverio Yousaf, Sultaan Lepsik, Martin Kinsinger, Thorsten Hirsch, Anna K H Imberty, Anne
Zahorska, Eva
Kuhaudomlarp, Sakonwan
Minervini, Saverio
Yousaf, Sultaan
Lepsik, Martin
Kinsinger, Thorsten
Hirsch, Anna K H
Imberty, Anne
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2020-07-06
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Abstract
Chronic infections with Pseudomonas aeruginosa are associated with the formation of bacterial biofilms. The tetrameric P. aeruginosa lectin LecA is a virulence factor and an anti-biofilm drug target. Increasing the overall binding affinity by multivalent presentation of binding epitopes can enhance the weak carbohydrate-ligand interactions. Low-nanomolar divalent LecA ligands/inhibitors with up to 260-fold valency-normalized potency boost and excellent selectivity over human galectin-1 were synthesized from d-galactose pentaacetate and benzaldehyde-based linkers in four linear steps.
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Chem Commun (Camb). 2020 Aug 4;56(62):8822-8825. doi: 10.1039/d0cc03490h.
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Article
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en
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1364-548X
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Attribution-NonCommercial-ShareAlike 4.0 International