title: High-throughput screening for inhibitors of sialyl- and fucosyltransferases.
abstract: Sweet screens: A high-throughput screening platform for identification of inhibitors of sialyl- and fucosyltransferases based on fluorescence polarization (FP) has been developed. An analogue of the natural donor substrate carrying a fluorescent label (green star) is transferred to a glycoprotein acceptor, which results in robust FP. The screening of 16,000 compounds against different glycosyltransferases has identified various interesting inhibitors.
authors.affiliation: Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA.
authors.forename: Cory D
authors.initials: CD
authors.lastname: Rillahan
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Brown
authors.forename: Amy C
authors.initials: AC
authors.lastname: Register
authors.forename: Hugh
authors.initials: H
authors.lastname: Rosen
authors.forename: James C
authors.initials: JC
authors.lastname: Paulson
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005647:Fucosyltransferases / Q000037:antagonists & inhibitors*; D057166:High-Throughput Screening Assays; D015394:Molecular Structure; D012799:Sialyltransferases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D005647:Fucosyltransferases; D012799:Sialyltransferases
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