Vanoxonin, a new inhibitor of thymidylate synthetase. III. Inhibition of thymidylate synthetase by vanoxonin-vanadium complex.
Quinquevalent vanadium complex with two mol of vanoxonin ligated by the two catechols was shown to be the active structure for inhibition of thymidylate synthetase. The catechol group of vanoxonin as the essential moiety for the inhibition of enzyme was further confirmed by studies of structure-activity relationships using the enzyme obtained from Ehrlich ascites carcinoma cells of mice. Vanoxonin-vanadium complex showed competitive inhibition with respect to deoxyuridylic acid but uncompetitive to 5,10-methylenetetrahydrofolate.
D004151:Dipeptides / Q000494:pharmacology*; D007700:Kinetics; D008780:Methyltransferases / Q000037:antagonists & inhibitors*; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*; D014639:Vanadium / Q000494:pharmacology*
D004151:Dipeptides; D014639:Vanadium; C038755:vanoxonin; D008780:Methyltransferases; D013940:Thymidylate Synthase