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OGA inhibition by GlcNAc-selenazoline

TitleOGA inhibition by GlcNAc-selenazoline
Publication TypeJournal Article
Year of Publication2010
AuthorsKim, EJu, Love, DC, Darout, E, Abdo, M, Rempel, B, Withers, SG, Rablen, PR, Hanover, JA, Knapp, S
JournalBIOORGANIC & MEDICINAL CHEMISTRY
Volume18
Pagination7058-7064
Date PublishedOCT 1
ISSN0968-0896
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. (C) 2010 Elsevier Ltd. All rights reserved.

DOI10.1016/j.bmc.2010.08.010