High-throughput screening for inhibitors of sialyl- and fucosyltransferases

Angew Chem Int Ed Engl. 2011 Dec 23;50(52):12534-7. doi: 10.1002/anie.201105065. Epub 2011 Nov 9.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Fucosyltransferases / antagonists & inhibitors*
  • High-Throughput Screening Assays*
  • Molecular Structure
  • Sialyltransferases / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Fucosyltransferases
  • Sialyltransferases