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Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase.
- 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.)
- Subjects :
- Humans
Hexosaminidases
Glycosylation
beta-N-Acetylhexosaminidases
Alzheimer Disease
Subjects
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