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Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside.

Authors :
Girardi B
Manna M
Van Klaveren S
Tomašič T
Jakopin Ž
Leffler H
Nilsson UJ
Ricklin D
Mravljak J
Schwardt O
Anderluh M
Source :
ChemMedChem [ChemMedChem] 2022 Feb 04; Vol. 17 (3), pp. e202100514. Date of Electronic Publication: 2021 Oct 06.
Publication Year :
2022

Abstract

Galectin-8 has gained attention as a potential new pharmacological target for the treatment of various diseases, including cancer, inflammation, and disorders associated with bone mass reduction. To that end, new molecular probes are needed in order to better understand its role and its functions. Herein we aimed to improve the affinity and target selectivity of a recently published galectin-8 ligand, 3-O-[1-carboxyethyl]-β-d-galactopyranoside, by introducing modifications at positions 1 and 3 of the galactose. Affinity data measured by fluorescence polarization show that the most potent compound reached a K <subscript>D</subscript> of 12 μM. Furthermore, reasonable selectivity versus other galectins was achieved, making the highlighted compound a promising lead for the development of new selective and potent ligands for galectin-8 as molecular probes to examine the protein's role in cell-based and in vivo studies.<br /> (© 2021 Wiley-VCH GmbH.)

Details

Language :
English
ISSN :
1860-7187
Volume :
17
Issue :
3
Database :
MEDLINE
Journal :
ChemMedChem
Publication Type :
Academic Journal
Accession number :
34613662
Full Text :
https://doi.org/10.1002/cmdc.202100514