Diaminocyclopentane-derived O-GlcNAcase inhibitors for combating tau hyperphosphorylation in Alzheimer’s disease
We developed potent and selective aminocyclopentane-derived inhibitors of human O–N-acetyl-β-D-glucosaminidase (OGA) implicated in Alzheimer’s disease. For example compound 13 was a nanomolar OGA inhibitor with 92 000-fold selectivity over human HexB. It was non-toxic and increased protein O-GlcNAcylation in the culture of murine neural cells, showing new alternatives in the treatment of tauopathies.
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