Folate Analogues as Substrates of Mammalian Folylpolyglutamate Synthetase

@article{Schoo1985FolateAA,
  title={Folate Analogues as Substrates of Mammalian Folylpolyglutamate Synthetase},
  author={M M Schoo and Zdenek B. Pristupa and Philip J. Vickers and K G Scrimgeour},
  journal={Cancer research},
  year={1985},
  volume={45 7},
  pages={3034-41}
}
The antifolate drugs methotrexate (MTX) and aminopterin (AM) have been tested as substrates for folylpolyglutamate synthetase (FPGS) partially purified from beef liver. The Km for MTX is 100 microM, and that for AM is 25 microM. These values are considerably higher than those for either tetrahydrofolate or folinic acid. Based on their ratios of Vmax to Km, AM is a better substrate than is MTX for the beef liver FPGS. Both are poorer substrates than tetrahydrofolate. The 7-hydroxy metabolites of… CONTINUE READING

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