Selective Monovalent Galectin-8 Ligands Based on 3-Lactoylgalactoside

被引：6

作者：

Girardi, Benedetta ^{[1
,2
]}

Manna, Martina ^{[1
]}

Van Klaveren, Sjors ^{[1
,3
]}

Tomasic, Tihomir ^{[1
]}

Jakopin, Ziga ^{[1
]}

Leffler, Hakon ^{[3
]}

Nilsson, Ulf J. ^{[3
]}

Ricklin, Daniel ^{[2
]}

Mravljak, Janez ^{[1
]}

Schwardt, Oliver ^{[2
]}

Anderluh, Marko ^{[1
]}

机构：

[1] Univ Ljubljana, Fac Pharm, Askerceva Cesta 7, Ljubljana 1000, Slovenia

[2] Univ Basel, Dept Pharmaceut Sci, Klingelbergstr 50, CH-4056 Basel, Switzerland

[3] Lund Univ, Dept Chem, Ctr Anal & Synth, Box 124, S-22100 Lund, Sweden

来源：

CHEMMEDCHEM | 2022年 / 17卷 / 03期

关键词：

galectins; galectin-8; carbohydrates; fluorescence polarization; molecular probes; GLYCOMIMETICS; AFFINITY; LECTIN;

D O I：

10.1002/cmdc.202100514

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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]-beta-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 mu M. 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.

引用

页数：7

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