Human Neuraminidases: Structures and Stereoselective Inhibitors.
Fiche publication
Date publication
février 2022
Journal
Journal of medicinal chemistry
Auteurs
Membres identifiés du Cancéropôle Est :
Dr BOURGUET Erika
Tous les auteurs :
Bourguet E, Figurska S, Fra Czek MM
Lien Pubmed
Résumé
This Perspective describes the classification, structures, substrates, mechanisms of action, and implications of human neuraminidases (hNEUs) in various pathologies. Some inhibitors have been developed for each isoform, leading to more precise interactions with hNEUs. Although crystal structure data are available for NEU2, most of the findings are based on NEU1 inhibition, and limited information is available for other hNEUs. Therefore, the synthesis of new compounds would facilitate the enrichment of the arsenal of inhibitors to better understand the roles of hNEUs and their mechanisms of action. Nevertheless, due to the already known inhibitors of human neuraminidase enzymes, a structure-activity relationship is presented along with different approaches to inhibit these enzymes for the development of potent and selective inhibitors. Among the different emerging strategies, one is the inhibition of the dimerization of NEU1 or NEU3, and the second is the inhibition of certain receptors located close to hNEU.
Référence
J Med Chem. 2022 Feb 16;: