The methotrexate story: a paradigm for development of cancer chemotherapeutic agents.

@article{Huennekens1994TheMS,
  title={The methotrexate story: a paradigm for development of cancer chemotherapeutic agents.},
  author={F. M. Huennekens},
  journal={Advances in enzyme regulation},
  year={1994},
  volume={34},
  pages={397-419}
}
Methotrexate (MTX), one of the earliest cancer chemotherapy agents, continues to be used extensively in the treatment of leukemia and a variety of other tumors. The efficacy of this drug results from its facile uptake by cells, rapid polyglutamylation and virtually stoichiometric inhibition of dihydrofolate reductase (DHFR), a key enzyme in cell replication. From the work of a multitude of biochemists, molecular biologists, organic chemists and pharmacologists, much is known about the mode of… CONTINUE READING

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