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

We report 5-substituted uridine derivatives as novel, uncharged inhibitors of ß-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.