title: Studies on the inhibition of sialyl- and galactosyltransferases.
abstract: The inhibition of the alpha-2,6-sialyltransferase from rat liver, the alpha-2,3-sialyltransferase from porcine submandibular gland and of the galactosyltransferase from human milk were studied using monosaccharide-, nucleoside- and nucleotide-derivatives of their naturally occurring donor substrates cytidine 5'-monophosphate-N-acetylneuraminic acid and uridine 5'-diphosphate-galactose, respectively. Only the corresponding nucleosides/nucleotides showed inhibitory activity. Periodate oxidation of CMP or CMP-Neu5Ac and of UMP or UDP-Gal led to reduced inhibitory efficiency with the respective transferase. The type and reversibility of the inhibition of some of these compounds, as well as the corresponding Ki values were determined.
authors.affiliation: Biochemisches Institut, Christian-Albrechts-Universität, Kiel, Germany.
authors.forename: R G
authors.initials: RG
authors.lastname: Kleineidam
authors.forename: T
authors.initials: T
authors.lastname: Schmelter
authors.forename: R T
authors.initials: RT
authors.lastname: Schwarz
authors.forename: R
authors.initials: R
authors.lastname: Schauer
mesh_terms: D000818:Animals; D001894:Borohydrides / Q000737:chemistry / Q000378:metabolism; D003568:Cytidine Monophosphate / Q000031:analogs & derivatives / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D005690:Galactose / Q000737:chemistry / Q000378:metabolism; D005700:Galactosyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006023:Glycoproteins / Q000378:metabolism*; D006031:Glycosylation; D006801:Humans; D007700:Kinetics; D008099:Liver / Q000201:enzymology; D008892:Milk / Q000201:enzymology; D009705:Nucleosides / Q000737:chemistry / Q000378:metabolism; D009711:Nucleotides / Q000737:chemistry / Q000378:metabolism; D010084:Oxidation-Reduction; D010504:Periodic Acid / Q000737:chemistry; D051381:Rats; D012794:Sialic Acids / Q000737:chemistry / Q000378:metabolism; D012799:Sialyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013363:Submandibular Gland / Q000201:enzymology; D013379:Substrate Specificity; D000094802:beta-D-Galactoside alpha 2-6-Sialyltransferase; D000094663:beta-Galactoside alpha-2,3-Sialyltransferase
chemical_list: D001894:Borohydrides; D004791:Enzyme Inhibitors; D006023:Glycoproteins; D009705:Nucleosides; D009711:Nucleotides; D012794:Sialic Acids; D010504:Periodic Acid; C025364:sodium borohydride; C009288:metaperiodate; D005700:Galactosyltransferases; D012799:Sialyltransferases; D003568:Cytidine Monophosphate; D005690:Galactose; D000094802:beta-D-Galactoside alpha 2-6-Sialyltransferase; D000094663:beta-Galactoside alpha-2,3-Sialyltransferase