High‐Throughput Screening for Inhibitors of Sialyl‐ and Fucosyltransferases

Sweet Screens: The promiscuity of sialyl- and fucosyltransferases has been exploited to develop a high-throughput screening (HTS) platform wherein transfer of a fluorescent analog of the natural donor substrate to a glycoprotein acceptor results in a robust fluorescence polarization readout. The use of this method to screen 16,000 compounds against 5 different glycosyltransferases has identified a panel of interesting inhibitors.