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Selective Monovalent Galectin‐8 Ligands Based on 3‐Lactoylgalactoside
Author(s) -
Girardi Benedetta,
Manna Martina,
Van Klaveren Sjors,
Tomašič Tihomir,
Jakopin Žiga,
Leffler Hakon,
Nilsson Ulf J.,
Ricklin Daniel,
Mravljak Janez,
Schwardt Oliver,
Anderluh Marko
Publication year - 2022
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100514
Subject(s) - galectin , chemistry , in vivo , selectivity , ligand (biochemistry) , galectin 1 , computational biology , galactose , target protein , combinatorial chemistry , binding selectivity , biochemistry , biophysics , cancer research , biology , receptor , microbiology and biotechnology , gene , catalysis
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 D 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.