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
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Research Support, Non-U.S. Gov't
MeSH terms
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Galactosyltransferases / antagonists & inhibitors*
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Galactosyltransferases / metabolism
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Humans
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Membrane Glycoproteins / antagonists & inhibitors
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Membrane Glycoproteins / biosynthesis
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Molecular Structure
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Monocytes / drug effects
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Monocytes / metabolism
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Structure-Activity Relationship
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Uridine / analogs & derivatives
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Uridine / chemistry
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Uridine / pharmacology*
Substances
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Enzyme Inhibitors
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Membrane Glycoproteins
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P-selectin ligand protein
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Galactosyltransferases
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Uridine