High-throughput identification of fucosyltransferase inhibitors using carbohydrate microarrays

Inhibitors to fucosyltransferase were screened in a high-throughput manner using a noncovalent carbohydrate microarray strategy and four nanomolar inhibitors were identified. A noncovalent carbohydrate microarray was used to screen for possible inhibitors to fucosyltransferases, which are critical to the synthesis of inflammation mediators like sialyl Lewis x (SLe x). Inhibition was followed by observation of the transferred fucose on the carbohydrate array with the lectin Tetragonolobus purpureas. Of these compounds, four inhibitors with nanomolar K is were discovered, with three of the top five inhibitors exhibiting a common architecture.