GlcNAcstatin C is a competitive nanomolar inhibitor of O-GlcNAcase enzymes which binds to the O-GlcNAcase active site by mimicking the transition state as revealed by X-ray crystallography. This compound is able to raise O-GlcNAc levels in human HEK 293 and SH-SY5Y neuroblastoma cell lines, providing a potent tool for the study of the role of O-GlcNAc in intracellular signal transduction pathways.
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- H.C. Dorfmueller, V.S. Borodkin, M. Schimpl, S.M. Shephed, N.A. Shpiro and D.M.F. van Aalten, "GlcNAcstatin: a picomolar, selective O-GlcNAcase inhibitor that modulates intracellular O-GlcNAcylation levels", J Am Chem Soc (2006), 128, 16484–16485. [PubMed] [Reprint]
- H.C. Dorfmueller, V.S. Borodkin, M. Schimpl and D.M.F. van Aalten, "GlcNAcstatins are nanomolar inhibitors of human O-GlcNAcase inducing cellular hyper-O-GlcNAcylation", Biochem J (2009), 420, 221–227. [PubMed] [Reprint]
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