GlcNAcstatin: a Picomolar,Selective O-GlcNAcase Inhibitor That Modulates Intracellular O-GlcNAcylation Levels

摘要

Many proteins in the eukaryotic cell are modified by O-linked N-acetylglucosamine (O-GlcNAc) on serines and threonines.O-GlcNAcylation has been shown to be important for regulation of the cell cycle,DNA transcription and translation,insulin sensitivity,and protein degradation.Misregulation of O-GlcNA-cylation is associated with diabetes and Alzheimer's disease.Two enzymes are involved in the dynamic cycling of this posttranslational modification,the O-GlcNAc transferase (OGT,classified as CAZY family GT41) and O-GlcNAcase (OGA,GH84).