Identification of O-Glc NAc Transferase Inhibitors(RMI)

Harvard University (Medical School), Boston MA

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Abstract

[unreadable] DESCRIPTION (provided by applicant): The goal of this project is to implement a developed donor displacement assay for O-GlcNAc transferase (OGT) in high throughput format using the MLSCN. OGT is the sole enzyme that mediates the attachment of O-GlcNAc groups to serine and threonine residues in the nucleus and cytoplasm of eukaryotic cells, and no specific inhibitors are known. This type of glycosylation is involved in signal transduction and plays a key role in many essential cellular processes. High O-GlcNAc levels have been correlated to insulin resistance and type 2 diabetes. In addition to elucidating the role of O-GlcNAc in cellular processes, inhibitors of OGT might be useful in studying and perhaps treating type 2 diabetes. [unreadable] [unreadable]