title: Uncharged nucleoside inhibitors of β-1,4-galactosyltransferase with activity in cells.
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.
authors.affiliation: Department of Chemistry, King's College London, Faculty of Natural & Mathematical Sciences, Britannia House, 7 Trinity Street, London, SE1 1DB, UK. gerd.wagner@kcl.ac.uk.
authors.forename: Jingqian
authors.initials: J
authors.lastname: Jiang
authors.forename: Varsha
authors.initials: V
authors.lastname: Kanabar
authors.forename: Beatriz
authors.initials: B
authors.lastname: Padilla
authors.forename: Francis
authors.initials: F
authors.lastname: Man
authors.forename: Simon C
authors.initials: SC
authors.lastname: Pitchford
authors.forename: Clive P
authors.initials: CP
authors.lastname: Page
authors.forename: Gerd K
authors.initials: GK
authors.lastname: Wagner
mesh_terms: D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D005700:Galactosyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008562:Membrane Glycoproteins / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D015394:Molecular Structure; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship; D014529:Uridine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D008562:Membrane Glycoproteins; C084882:P-selectin ligand protein; D005700:Galactosyltransferases; D014529:Uridine