Cell cycle effects of antifolate antimetabolites: implications for cytotoxicity and cytostasis

@article{Tonkinson1997CellCE,
  title={Cell cycle effects of antifolate antimetabolites: implications for cytotoxicity and cytostasis},
  author={John L. Tonkinson and Philip Marder and Sherri L. Andis and Richard M Schultz and Lynn S. Gossett and C -Y.T. Shih and Laurane G. Mendelsohn},
  journal={Cancer Chemotherapy and Pharmacology},
  year={1997},
  volume={39},
  pages={521-531}
}
 Purpose: Cell cycle-related events in CCRF-CEM lymphocytic leukemia cells were examined subsequent to inhibition of thymidylate synthase (TS) or GAR formyltransferase (GARFT) and prior to cell death or stasis. Methods: Cell populations were treated with the GARFT inhibitors 6R-5,10-dideazatetrahydrofolate (lometrexol) or LY309887, the TS inhibitor ZD1694, or the multitargeted antifolate LY231514. DNA content, nucleoside precursor incorporation and proliferating cell nuclear antigen (PCNA… CONTINUE READING
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4 Excerpts

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LY231514 and its polyglutamates exhibit potent inhibition against both human dihydrofolate reductase (DHFR) and thymidylate synthase (TS): multiple folate enzymes inhibition

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