OGA inhibition by GlcNAc-selenazoline

The title compound, which differs from the powerful O-GlcNAcase (OGA) inhibitor GlcNAc-thiazoline only at the chalcogen atom (Se for S), is a much weaker inhibitor in a direct OGA assay. In human cells, however, the selenazoline shows comparable ability to induce hyper-O-GlcNAc-ylation, and the two...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2010-10, Vol.18 (19), p.7058-7064
Hauptverfasser: Kim, Eun Ju, Love, Dona C., Darout, Etzer, Abdo, Mohannad, Rempel, Brian, Withers, Stephen G., Rablen, Paul R., Hanover, John A., Knapp, Spencer
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Sprache:eng
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Zusammenfassung:The title compound, which differs from the powerful O-GlcNAcase (OGA) inhibitor GlcNAc-thiazoline only at the chalcogen atom (Se for S), is a much weaker inhibitor in a direct OGA assay. In human cells, however, the selenazoline shows comparable ability to induce hyper-O-GlcNAc-ylation, and the two show similar reduction of insulin-stimulated translocation of glucose transporter 4 in differentiated 3T3 adipocytes.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2010.08.010