Recent preclinical and clinical studies with the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB 3717).

@article{Calvert1987RecentPA,
  title={Recent preclinical and clinical studies with the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB 3717).},
  author={Alan Hilary Calvert and David R. Newell and Ann L. Jackman and Lindsey A. Gumbrell and Edward R. Sikora and Barbara Grzelakowska-Sztabert and Justin A Bishop and Ian Judson and S. J. Harland and Kenneth R. Harrap},
  journal={NCI monographs : a publication of the National Cancer Institute},
  year={1987},
  volume={5},
  pages={213-8}
}
CB 3717, N10-propargyl-5,8-dideazafolic acid, is a tight-binding inhibitor of thymidylate synthase (TS) whose cytotoxicity is mediated solely through the inhibition of this enzyme. Recent preclinical studies have focused on the intracellular formation of CB 3717 polyglutamates. Following a 12-hour exposure of L1210 cells to 50 microM [3H]CB 3717, 30% of the extractable radioactivity could be accounted for as CB 3717 tetra- and pentaglutamate, as determined by high-pressure liquid chromatography… CONTINUE READING

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