2 research outputs found
A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d-galactose pentaacetate
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. Lownanomolar 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
A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d-galactose pentaacetate.
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