ChemComm 58, 63, 8838-8841 (2022)

10 srpna, 2022 10:47 am Published by Leave your thoughts

IF 6,065

Diaminocyclopentane-derived O-GlcNAcase inhibitors for combating tau hyperphosphorylation in Alzheimer’s disease

Weber Patrick, Mészáros Zuzana, Jagečić Denis, Hribljan Valentina, Mitrečić Dinko, Bojarová PavlaSlámová Kristýna, Vrba Jiří, Kulik Natalia, Křen Vladimír, Stütz E. Arnold

 Abstract

We developed potent and selective aminocyclopentane-derived inhibitors of human ON-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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