GlcNAcstatin G is a nanomolar inhibitor of human OGA that is 900,000-fold selective for HsOGA compared to the related lysosomal hexosaminidases. When used at nanomolar concentrations on live cells, this cell-penetrant molecule shifts the O-GlcNAc equilibrium toward hyper-O-GlcNAcylation with EC50 values reported in the 20–100 nM range.
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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]
- H.C. Dorfmueller, V.S. Borodkin, M. Schimpl, X. Zheng, R. Kime, K.D. Read and D.M.F. van Aalten, "Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases", Chem Biol (2010), 17, 1250–1255. [PubMed] [Reprint]
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