Article on lectin-inhibitors published in ChemMedChem

Karolina and Joe’s review article on “Structural considerations for building synthetic glycoconjugates as inhibitors for Pseudomonas aeruginosa lectins” has been published by ChemMedChem. The article is available here: https://doi.org/10.1002/cmdc.202200081

Pseudomonas aeruginosa is a pathogenic bacterium, responsible for a large portion of nosocomial infections globally and designated as critical priority by the World Health Organisation. Its characteristic carbohydrate-binding proteins LecA and LecB, which play a role in biofilm-formation and lung-infection, can be targeted by glycoconjugates. In the review, we present the wide range of inhibitors for these proteins (136 references), highlighting structural features and which impact binding affinity and/or therapeutic effects, including carbohydrate selection; linker length and rigidity; and scaffold topology, particularly for multivalent candidates. We also discuss emerging therapeutic strategies, which build on targeting of LecA and LecB, such as anti-biofilm activity, anti-adhesion and drug-delivery, with promising prospects for medicinal chemistry.

This article would be a good entry-point for any researchers considering tackling P. aeruginosa as a target organism, particularly if they want to build lectin-targeting ligands building on the existing consensus in the field on the best structural features to ensure high lectin affinity.

Thanks to Science Foundation Ireland for funding this research.