Diaminocyclopentane - l-Lysine Adducts: Potent and selective inhibitors of human O-GlcNAcase.
Bioorg Chem
; 148: 107452, 2024 Jul.
Article
in En
| MEDLINE
| ID: mdl-38763001
ABSTRACT
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Enzyme Inhibitors
/
Lysine
Limits:
Humans
Language:
En
Journal:
Bioorg Chem
Year:
2024
Document type:
Article
Country of publication: