Biochemical evidence for the role of alkyl-lysophospholipids on liver sialyltransferase.
Antineoplastic alkyl-lysophospholipids were found to exert a strong inhibitory effect on membranous or solubilized asialomucin-sialyltransferase (CMP-N-acetylneuraminate: D-galactosyl-glycoprotein N-acetylneuraminyltransferase, EC 2.4.99.1) activity. This inhibitory effect was dependent on the presence of the choline moiety in position 3 of the glycerol molecule, as well as on the presence of long ether-linked aliphatic side chain in position 1 and the absence of any large substituent in position 2. As an example, 1-octadecyl-2-O-methyl-glycero-3-phosphorylcholine acted as a mixed-type inhibitor. Such an inhibitory process on sialyltransferase activity might be an additional factor in the tumor cell destructive effect of alkyl-lysophospholipids.
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007700:Kinetics; D008099:Liver / Q000201:enzymology*; D008244:Lysophosphatidylcholines / Q000494:pharmacology; D008246:Lysophospholipids; D051379:Mice; D008815:Mice, Inbred Strains; D010742:Phospholipid Ethers; D010743:Phospholipids / Q000494:pharmacology*; D012799:Sialyltransferases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014166:Transferases / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D008244:Lysophosphatidylcholines; D008246:Lysophospholipids; D010742:Phospholipid Ethers; D010743:Phospholipids; C026659:edelfosine; D014166:Transferases; D012799:Sialyltransferases