Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8
Copyright policy )Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8
A series of O2 and O3-derivatized methyl beta-d-talopyranosides were synthesized and evaluated in vitro as inhibitors of the galactose-binding galectin-1, -2, -3, -4 (N- and C-terminal domains), 8 (N-terminal domain), and 9 (N-terminal domain). Galectin-4C and 8N were found to prefer the d-talopyranose configuration to the natural ligand d-galactopyranose configuration. Derivatization at talose O2 and/or O3 provided selective submillimolar inhibitors for these two galectins.
- Griffith University Australia
- Lund University Sweden
Binding Sites, Galectin 1, Galectin 3, Galectins, Galectin 4, Organic chemistry, Galactose, Ligands, Protein Engineering, Benzoates, Protein Structure, Tertiary, Lactones, Pharmacology and pharmaceutical sciences, Spectrometry, Fluorescence, Models, Chemical, Medicinal and biomolecular chemistry, Humans, Glycosides, Pyrans
Binding Sites, Galectin 1, Galectin 3, Galectins, Galectin 4, Organic chemistry, Galactose, Ligands, Protein Engineering, Benzoates, Protein Structure, Tertiary, Lactones, Pharmacology and pharmaceutical sciences, Spectrometry, Fluorescence, Models, Chemical, Medicinal and biomolecular chemistry, Humans, Glycosides, Pyrans
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