A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d-galactose pentaacetate.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
Hirsch, Anna K H
MetadataShow full item record
AbstractChronic 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.
CitationChem Commun (Camb). 2020 Aug 4;56(62):8822-8825. doi: 10.1039/d0cc03490h.
AffiliationHIPS, Helmholtz-Institut für Pharmazeutische Forschung Saarland, Universitätscampus E8.1 66123 Saarbrücken, Germany.
PublisherRoyal Sciety of Chemistry
The following license files are associated with this item:
- Creative Commons
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-ShareAlike 4.0 International
- Toward the Rational Design of Galactosylated Glycoclusters That Target Pseudomonas aeruginosa Lectin A (LecA): Influence of Linker Arms That Lead to Low-Nanomolar Multivalent Ligands.
- Authors: Wang S, Dupin L, Noël M, Carroux CJ, Renaud L, Géhin T, Meyer A, Souteyrand E, Vasseur JJ, Vergoten G, Chevolot Y, Morvan F, Vidal S
- Issue date: 2016 Aug 8
- Development and optimization of a competitive binding assay for the galactophilic low affinity lectin LecA from Pseudomonas aeruginosa.
- Authors: Joachim I, Rikker S, Hauck D, Ponader D, Boden S, Sommer R, Hartmann L, Titz A
- Issue date: 2016 Aug 16
- Design and Synthesis of Galactosylated Bifurcated Ligands with Nanomolar Affinity for Lectin LecA from Pseudomonas aeruginosa.
- Authors: Angeli A, Li M, Dupin L, Vergoten G, Noël M, Madaoui M, Wang S, Meyer A, Géhin T, Vidal S, Vasseur JJ, Chevolot Y, Morvan F
- Issue date: 2017 Jun 1
- Synthesis of multivalent carbohydrate-centered glycoclusters as nanomolar ligands of the bacterial lectin LecA from Pseudomonas aeruginosa.
- Authors: Gening ML, Titov DV, Cecioni S, Audfray A, Gerbst AG, Tsvetkov YE, Krylov VB, Imberty A, Nifantiev NE, Vidal S
- Issue date: 2013 Jul 8
- Development of Pseudomonas aeruginosa Lectin LecA Inhibitor by using Bivalent Galactosides Supported on Polyproline Peptide Scaffolds.
- Authors: Huang SF, Lin CH, Lai YT, Tsai CL, Cheng TR, Wang SK
- Issue date: 2018 Mar 16