Titre :

Comparative analysis of sulfated and sulfonated disaccharide analogs as TLR4 modulators and heparanase inhibitors

Auteur(s) :

El-Abid, Jamal [Auteur]
Koffi Teki, Dindet Steve-Evanes K. L. C. [Auteur]
Bil, Abed [Auteur]
Denys, Agnes [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Vallin, Aurélie [Auteur]
Lefebvre, Corentin [Auteur]
Allain, Fabrice [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Chagnault, Vincent [Auteur]
Kovensky, José [Auteur]

Titre de la revue :

New Journal of Chemistry

Nom court de la revue :

New J. Chem.

Numéro :

48

Pagination :

9559-9566

Éditeur :

Royal Society of Chemistry

Date de publication :

2024-04-26

ISSN :

1144-0546

Mot(s)-clé(s) en anglais :

Toll-like receptors
III Binding domain
Endogenous ligands
Drosophila
Immunity
Heparin

Discipline(s) HAL :

Sciences du Vivant [q-bio]
Chimie/Chimie théorique et/ou physique

Résumé en anglais : [en]

This article delves into the synthesis and biological evaluation of sulfated and sulfonated disaccharide analogs, exploring their interactions with toll-like receptor 4 (TLR4) and their potential as drug candidates for ...
Lire la suite >This article delves into the synthesis and biological evaluation of sulfated and sulfonated disaccharide analogs, exploring their interactions with toll-like receptor 4 (TLR4) and their potential as drug candidates for inflammatory diseases. A significant aspect of the study is the examination of these analogs as inhibitors of heparanase, an enzyme that cleaves glycosidic linkages in heparan sulfate, producing proinflammatory fragments that activate TLR4. The research presents a comparative analysis of sulfate and sulfonate groups in these compounds, evaluating their synthesis, biological activity, and specific roles in TLR4-mediated immune responses, with a particular focus on their ability to modulate heparanase activity. Compound 9 (6,6′-disulfonated disaccharide from methyl cellobioside) emerged as a potent TLR4 activator and a promising candidate for inflammatory drug development, exhibiting notable specificity and efficacy. The IC50 values for heparanase inhibition varied, highlighting distinct efficacy profiles for sulfonated and sulfated analogs, with cellobiose derivatives showing notable differences in inhibition capabilities.Lire moins >

Langue :

Anglais

Comité de lecture :

Oui

Audience :

Internationale

Vulgarisation :

Non

Établissement(s) :

Université de Lille
CNRS

Collections :

• Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576

Équipe(s) de recherche :

Diversité structurale des héparanes sulfates et régulation de la réponse inflammatoire

Date de dépôt :

2025-01-20T12:52:58Z
2025-01-23T14:28:50Z