Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase.
Alzheimer’s disease
Diaminocyclopentane
Glycosidase inhibition
O-GlcNAcase
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
11 2023
11 2023
Historique:
received:
15
05
2023
revised:
11
08
2023
accepted:
27
08
2023
medline:
18
9
2023
pubmed:
5
9
2023
entrez:
4
9
2023
Statut:
ppublish
Résumé
A new class of compounds inhibiting de-O-glycosylation of proteins has been identified. Highly substituted diaminocyclopentanes are impressively selective reversible non-transition state O-β-N-acetyl-d-glucosaminidase (O-GlcNAcase) inhibitors. The ease of preparative access and remarkable biological activities provide highly viable leads for the development of anti-tau-phosphorylation agents with a view to eventually ameliorating Alzheimer's disease.
Identifiants
pubmed: 37666109
pii: S0045-2068(23)00480-7
doi: 10.1016/j.bioorg.2023.106819
pii:
doi:
Substances chimiques
hexosaminidase C
EC 3.2.1.50
beta-N-Acetylhexosaminidases
EC 3.2.1.52
Hexosaminidases
EC 3.2.1.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
106819Subventions
Organisme : Austrian Science Fund FWF
ID : I 5236
Pays : Austria
Informations de copyright
Copyright © 2023 The Author(s). Published by Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.