High-throughput identification of fucosyltransferase inhibitors using carbohydrate microarrays

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(j)s were discovered, with three of the top five inhibitors exhibiting a common architecture. (C) 2004 Elsevier Ltd. All rights reserved.