Diaminocyclopentane-derived <i>O</i>-GlcNAcase inhibitors for combating tau hyperphosphorylation in Alzheimer's disease (CROSBI ID 322228)
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Podaci o odgovornosti
Weber, Patrick ; Mészáros, Zuzana ; Jagečić, Denis ; Hribljan, Valentina ; Mitrečić, Dinko ; Bojarová, Pavla ; Slámová, Kristýna ; Vrba, Jiří ; Kulik, Natalia ; Křen, Vladimír ; Stütz, Arnold E.
engleski
Diaminocyclopentane-derived <i>O</i>-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.
Alzheimer, tau, O-GlcNAcase inhibitors
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Podaci o izdanju
Povezanost rada
Biotehnologija u biomedicini (prirodno područje, biomedicina i zdravstvo, biotehničko područje), Temeljne medicinske znanosti