Discovery of potent 1,1-diarylthiogalactoside glycomimetic inhibitors of Pseudomonas aeruginosa LecA with antibiofilm properties

carbohydrates, drug discovery,

This great research team recently presented a new series of 1,1-diarylthiogalactoside for targeting the Pseudomonas aeruginosa LecA. The highest affinity (Kd = 160 nM) was obtained for a divalent ligand containing two galactoside units. A monovalent ligand displayed high affinity toward LecA (Kd = 1 μM) and strong antibiofilm activity while others induced a significant antibiofilm activity with no associated bactericidal activity.
Alexandre Bruneau, Emilie Gillon, Aurélie Furiga, Etienne BRACHET, Mouad Alami, Christine Roques, Annabelle Varrot, Anne Imberty, Samir Messaoudi 

See the full article here: Discovery of potent 1,1-diarylthiogalactoside glycomimetic inhibitors of Pseudomonas aeruginosa LecA with antibiofilm properties

Targeting bacterial virulence as a novel treatment against AMR infections

drug development, ,

Have you known that Arivin Therapeutics uses cyclodextrin for targeting bacterial virulence as a novel treatment against AMR infections? Among their MoA claims, the following are listed:
– Targeting virulence factors is effective, also against extensively resistant isolates
– Targeting virulence avoids rapid resistance
– Direct reduction in inflammatory responses
– Potentiates the function of antibiotics
Also, there is a spectacular video about how CDs develop their effect as antibacterials.

https://arivintx.com/our-science

Using heparan sulfate octadecasaccharide (18-mer) as a multi-target agent to protect against sepsis

drug discovery,

Fascinating research from University of North Carolina at Chapel Hill, The State University of New York and Rensselaer Polytechnic Institute on using heparan sulfate octadecasaccharide (18-mer) as a multi-target agent to protect against sepsis.

Yongmei Xu, Katelyn Arnold, Fuming Zhang, Vijayakanth Pagadala, Robert Linhardt et al.

See the full article here.