Uncharged nucleoside inhibitors of β-1,4-galactosyltransferase with activity in cells

Chem Commun (Camb). 2016 Mar 11;52(20):3955-8. doi: 10.1039/c5cc09289b. Epub 2016 Feb 16.

Abstract

We report 5-substituted uridine derivatives as novel, uncharged inhibitors of β-1,4-galactosyltransferase and chemical tools for cellular applications. The new inhibitors reduce P-selectin glycoprotein 1 (PSGL-1) expression in human monocytes. Our results also provide novel insights into a unique mode of glycosyltransferase inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Galactosyltransferases / antagonists & inhibitors*
  • Galactosyltransferases / metabolism
  • Humans
  • Membrane Glycoproteins / antagonists & inhibitors
  • Membrane Glycoproteins / biosynthesis
  • Molecular Structure
  • Monocytes / drug effects
  • Monocytes / metabolism
  • Structure-Activity Relationship
  • Uridine / analogs & derivatives
  • Uridine / chemistry
  • Uridine / pharmacology*

Substances

  • Enzyme Inhibitors
  • Membrane Glycoproteins
  • P-selectin ligand protein
  • Galactosyltransferases
  • Uridine