Selection of Galectin-Binding Ligands from Synthetic Glycopeptide Libraries

0580153 - ÚOCHB 2025 RIV US eng J - Journal Article
Kovalová, Anna - Prouza, Vít - Zavřel, Martin - Hájek, Miroslav - Dzijak, Rastislav - Magdolenová, Alžbeta - Pohl, Radek - Voburka, Zdeněk - Parkan, Kamil - Vrábel, Milan
Selection of Galectin-Binding Ligands from Synthetic Glycopeptide Libraries.
ChemPlusChem. (2024), č. článku e202300567. ISSN 2192-6506. E-ISSN 2192-6506
R&D Projects: GA MŠMT(CZ) LX22NPO5104; GA ČR(CZ) GA22-17586S
EU Projects: European Commission(XE) 677465 - SWEETOOLS
Institutional support: RVO:61388963
Keywords : click chemistry * glycopeptide libraries * lectins * split-and-mix * sugars
OECD category: Organic chemistry
Impact factor: 3.4, year: 2022
Method of publishing: Open access
https://doi.org/10.1002/cplu.202300567

Galectins, a class of carbohydrate-binding proteins, play a crucial role in various physiological and disease processes. Therefore, the identification of ligands that efficiently bind these proteins could potentially lead to the development of new therapeutic compounds. In this study, we present a method that involves screening synthetic click glycopeptide libraries to identify lectin-binding ligands with low micromolar affinity. Our methodology, initially optimized using Concanavalin A, was subsequently applied to identify binders for the therapeutically relevant galectin 1. Binding affinities were assessed using various methods and showed that the selected glycopeptides exhibited enhanced binding potency to the target lectins compared to the starting sugar moieties. This approach offers an alternative means of discovering galectin-binding ligands as well as other carbohydrate-binding proteins, which are considered important therapeutic targets.
Permanent Link: https://hdl.handle.net/11104/0348915