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Diaminocyclopentane - l-Lysine Adducts: Potent and selective inhibitors of human O-GlcNAcase
P. Weber, P. Bojarová, J. Brouzdová, V. Křen, N. Kulik, AE. Stütz, M. Thonhofer, TM. Wrodnigg
Bioorganic chemistry.
2024 ;
148 (-) :
107452.
[pub] 20240518
Jazyk angličtina Země Spojené státy americké
Typ dokumentu časopisecké články
Perzistentní odkaz
https://www.medvik.cz/link/bmc24013361
- MeSH
- beta-N-acetylhexosaminidasy antagonisté a inhibitory metabolismus MeSH
- cyklopentany chemie farmakologie chemická syntéza MeSH
- inhibitory enzymů * chemie farmakologie chemická syntéza MeSH
- lidé MeSH
- lysin * chemie farmakologie MeSH
- molekulární struktura MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
A new class of compounds, namely highly substituted diaminocyclopentane-l-lysine adducts, have been discovered as potent inhibitors of O-GlcNAcase, an enzyme crucial for protein de-O-glycosylation. These inhibitors exhibit exceptional selectivity and reversibility and are the first example of human O-GlcNAcase inhibitors that are structurally related to the transition state of the rate-limiting step with the "aglycon" still in bond-length proximity. The ease of their preparation, remarkable biological activities, stability, and non-toxicity make them promising candidates for the development of anti-tau-phosphorylation agents holding significant potential for the treatment of Alzheimer's disease.
Citace poskytuje Crossref.org
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