期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 14, 期 13, 页码 3476-3481出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6ob00220j
关键词
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资金
- Universite Claude Bernard Lyon 1
- CNRS
- COST Action MultiGlycoNano [CM-1102]
- Labex ARCANE [ANR-11-LABX-003]
- Royal Society [JP090449]
- Region Rhone-Alpes (Cluster de Recherche Chimie)
- GDR Pseudomonas
Anti-adhesive glycoclusters offer potential as therapeutic alternatives to classical antibiotics in treating infections. Pillar[5]arenes functionalised with either five galactose or five fucose residues were readily prepared using CuAAC reactions and evaluated for their binding to three therapeutically relevant bacterial lectins: LecA and Lec B from Pseudomonas aeuruginosa and BambL from Burkholderia ambifaria. Steric interactions were demonstrated to be a key factor in achieving good binding to LecA with more flexible galactose glycoclusters showing enhanced activity. In contrast binding to the fucose-selective lectins confirmed the importance of topology of the glycoclusters for activity with the pillar[5]arene ligand proving a selective ligand for BambL.
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