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Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8

Journal Article


Abstract


  • A series of O2 and O3-derivatized methyl β-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. © 2008 Elsevier Ltd. All rights reserved.

Publication Date


  • 2008

Citation


  • Öberg, C. T., Blanchard, H., Leffler, H., & Nilsson, U. J. (2008). Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8. Bioorganic and Medicinal Chemistry Letters, 18(13), 3691-3694. doi:10.1016/j.bmcl.2008.05.066

Scopus Eid


  • 2-s2.0-44749093873

Start Page


  • 3691

End Page


  • 3694

Volume


  • 18

Issue


  • 13

Abstract


  • A series of O2 and O3-derivatized methyl β-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. © 2008 Elsevier Ltd. All rights reserved.

Publication Date


  • 2008

Citation


  • Öberg, C. T., Blanchard, H., Leffler, H., & Nilsson, U. J. (2008). Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8. Bioorganic and Medicinal Chemistry Letters, 18(13), 3691-3694. doi:10.1016/j.bmcl.2008.05.066

Scopus Eid


  • 2-s2.0-44749093873

Start Page


  • 3691

End Page


  • 3694

Volume


  • 18

Issue


  • 13