2020年7月10日 · As the antibiotic therapeutic strategy has become less effective in the treatment of uropathogen-related UTIs, the anti-adhesive molecules active against fimbrial adhesins, key determinants of urovirulence, are attractive alternatives. The best-characterized bacterial adhesin is FimH, produced by uropathogenic Escherichia coli (UPEC).

FimH ligand binding affinity of A. early synthetic mannosides B. oligomannose-9 and subunits and C. other sugars. Herein, we comprehensively review rational ligand design and drug discovery strategies which have been employed to generate high-affinity, monovalent inhibitors of FimH.

2018年2月2日 · To gain a detailed insight into the binding kinetics of the interaction of FimH with mannoside ligands, surface plasmon resonance (SPR) measurements were performed (Table 4). The carboxyl-functionalized mannoside 5 (see supporting information for structure and synthesis) was immobilized via an ethylenediamine linker on a CM4 chip.

2010年5月14日 · The Escherichia coli fimbrial adhesive protein, FimH, mediates shear-dependent binding to mannosylated surfaces via force-enhanced allosteric catch bonds, but the underlying structural mechanism was previously unknown.

2023年5月1日 · The binding affinities of dimannoses toward the FimH lectin have been determined using SPR, Molecular Mechanics Poisson-Boltzmann Surface Area (MM-PBSA) calculations, and a lectin profile kit, respectively.

2004年11月25日 · FimH is a two-domain adhesin protein at the end of the tip fibrillum, responsible for the mannose-sensitive bacterial adhesion. The amino-terminal lectin domain (residues 1–158) is joined to the carboxy-terminal pilin domain (residues 159–279) that links the adhesin to …

The solution equilibrium binding constants of FimH for most natural oligomannoside substructures, present in the glycan part of high-mannose glycoproteins , were characterized in an surface plasmon resonance (SPR) competition experiment .

2017年7月3日 · Affinities of FimH for O-linked alkene-(22–25), alkane-(26–29) and alkyne-(50–53) derivatized O-mannopyranosides, as measured in SPR and/or ITC experiments, and their minimal concentrations inhibiting haemagglutination (HAI).

2017年7月19日 · The binding of FimH adhesins to recombinant porcine CRT immobilized on CM5 sensor chips (GE Healthcare) was analyzed by SPR using a BIAcore T200. CRT immobilization level corresponds to approximately 150 RU.

The FimH type-1 fimbrial adhesin allows pathogenic Escherichia coli to adhere to glycoproteins in the epithelial linings of human bladder and intestinal tract, by using multiple fimbriae...