Screening Diverse Glycosyltransferases Using Homogenous, Fluorescent Transcreener HTS Assays for Direct Detection of Nucleotide Products

Glycosyltransferase enzymes participate in extremely diverse metabolic and regulatory roles by catalyzing the transfer of sugar molecules to protein, lipid and carbohydrate acceptors as well as endogenous and xenobiotic small molecules. From a drug discovery point of view, they are gaining increasing interest as targets for “substrate reduction therapy” in lysosomal storage diseases, and as anti-microbial targets for disrupting bacterial cell wall biosynthesis. This study indicates that a suite of Transcreener assays may be a powerful approach for screening and profiling diverse glycosyltransferases in humans.