Metal-binding cyclodextrins: Synthesis and complexation with Zn2+ and Ga3+ cations towards antimicrobial applications

carbohydrates,

The latest paper of our CSO, Milo Malanga resulted from a great collaboration with Marco Agnes, Gábor Benkovics, Georgios Miliotis, Dina Yannakopoulou, and several others, is just out!
We have prepared a family of cyclodextrins substituted with iminodiacetic acid (IDA) on their narrow side, while the wider side is either unmodified or per-2,3-O-methylated. The molecules form strong coordination complexes with Zn2+ or Ga3+ cations in aqueous solution. 50 μΜ of the compounds achieve complete re-sensitization of metallo-β-lactamase-producing Gram-negative clinical bacterial strains resistant to the carbapenems imipenem and meropenem.

Metal-binding cyclodextrins: Synthesis and complexation with Zn2+ and Ga3+ cations towards antimicrobial applications – ScienceDirect

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.