Plasmodium falciparum: inhibition of dolichol kinase by mefloquine.
Dolichol kinase, a rate limiting enzyme for the supply with dolichyl monophosphate as glycosyl carrier lipid, was demonstrated in Plasmodium falciparum. The enzyme was found to be associated with the pellet fraction and to depend on cytidine triphosphate as phosphoryl donor. The apparent Km values of the plasmodial enzyme were determined to be 0.8 mM for cytidine triphosphate and 17 micrograms ml-1 for dolichol. In the presence of 0.5 mM mefloquine, the inhibition of enzyme activity was found to be about 50%.
D000818:Animals; D037621:Artemisinins; D002413:Cations, Divalent; D002738:Chloroquine / Q000494:pharmacology; D003570:Cytidine Triphosphate / Q000378:metabolism; D003902:Detergents; D004286:Dolichols / Q000378:metabolism; D004533:Egtazic Acid / Q000494:pharmacology; D004912:Erythrocytes / Q000201:enzymology; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D015767:Mefloquine; D008861:Microsomes / Q000201:enzymology; D009711:Nucleotides / Q000378:metabolism; D010770:Phosphotransferases / Q000037:antagonists & inhibitors*; D017853:Phosphotransferases (Alcohol Group Acceptor); D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology*; D011804:Quinolines / Q000494:pharmacology*; D012717:Sesquiterpenes / Q000494:pharmacology; D014268:Trifluoperazine / Q000494:pharmacology
D037621:Artemisinins; D002413:Cations, Divalent; D003902:Detergents; D004286:Dolichols; D009711:Nucleotides; D011804:Quinolines; D012717:Sesquiterpenes; D014268:Trifluoperazine; D004533:Egtazic Acid; D003570:Cytidine Triphosphate; D002738:Chloroquine; C031327:artemisinin; D010770:Phosphotransferases; D017853:Phosphotransferases (Alcohol Group Acceptor); C020087:dolichol kinase; D015767:Mefloquine