OGA inhibition by GlcNAc-selenazoline

GlcNAc-硒唑啉抑制OGA

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作者:Eun Ju Kim, Dona C Love, Etzer Darout, Mohannad Abdo, Brian Rempel, Stephen G Withers, Paul R Rablen, John A Hanover, Spencer Knapp

Abstract

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.

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