期刊
BIOORGANIC CHEMISTRY
卷 112, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2021.104876
关键词
FimH adhesin; Anti-adhesive therapies; Anti-virulence; On-cell STD NMR; Carbohydrate-lectin interactions; Multivalent ligands; Ligand-receptor interaction studies; FimH ligand screening; Lectin-mediated adhesion inhibitors
资金
- MIUR [2017E44A9P]
The study developed an on-cell NMR method to screen FimH ligands and identify their binding epitopes. Testing was done in a physiological environment, aiming to develop new antiadhesive and diagnostic tools against urinary tract infection pathogens.
We describe the development of an on-cell NMR method for the rapid screening of FimH ligands and the structural identification of ligand binding epitopes. FimH is a mannose-binding bacterial adhesin expressed at the apical end of type 1 pili of uropathogenic bacterial strains and responsible for their D-mannose sensitive adhesion to host mammalian epithelial cells. Because of these properties, FimH is a key virulence factor and an attractive therapeutic target for urinary tract infection. We prepared synthetic D-mannose decorated dendrimers, we tested their ability to prevent the FimH-mediated yeast agglutination, and thus we used the compounds showing the best inhibitory activity as models of FimH multivalent ligands to set up our NMR methodology. Our experimental protocol, based on on-cell STD NMR techniques, is a suitable tool for the screening and the epitope mapping of FimH ligands aimed at the development of new antiadhesive and diagnostic tools against urinary tract infection pathogens. Notably, the study is carried out in a physiological environment, i.e. at the surface of living pathogen cells expressing FimH.
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