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Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase.

Authors :
Weber P
Mészáros Z
Bojarová P
Ebner M
Fischer R
Křen V
Kulik N
Müller P
Vlachová M
Slámová K
Stütz AE
Thonhofer M
Torvisco A
Wrodnigg TM
Wolfsgruber A
Source :
Bioorganic chemistry [Bioorg Chem] 2023 Nov; Vol. 140, pp. 106819. Date of Electronic Publication: 2023 Aug 28.
Publication Year :
2023

Abstract

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.<br />Competing Interests: 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.<br /> (Copyright © 2023 The Author(s). Published by Elsevier Inc. All rights reserved.)

Details

Language :
English
ISSN :
1090-2120
Volume :
140
Database :
MEDLINE
Journal :
Bioorganic chemistry
Publication Type :
Academic Journal
Accession number :
37666109
Full Text :
https://doi.org/10.1016/j.bioorg.2023.106819