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Folate Metabolites as Modulators of Antitumor Drug Activity

  • Chapter
Chemistry and Biology of Pteridines and Folates

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 338))

Abstract

[R,S]-5-formyltetrahydrofolate (5-CHOFH4) has shown significant potentiation of fluorouracil (FU) activity in colorectal, breast, and head and neck cancer.1–7 The biochemical basis for this enhanced activity is metabolic conversion of 5-CHOFH4 to 5,10-methylenetetrahydrofolate (CH2FH4) which in turn stabilizes the inhibitory complex formed between the active metabolite of fluorouracil, 5-fluoro-2-deoxyuridine-5’-monophosphate (FdUMP), and thymidylate synthase. This inhibition results in depletion of thymidylate required for DNA synthesis and repair.8–11

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Authors and Affiliations

  1. Department of Biochemistry and Molecular Biology, Medical University of South Carolina, Charleston, SC, 29425-2211, USA

    David G. Priest, John C. Schmitz & Marlene A. Bunni

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  1. David G. Priest
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  2. John C. Schmitz
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  3. Marlene A. Bunni
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Editor information

Editors and Affiliations

  1. Dept of Pharmacology College of Medicine, Universily of South Alabama, Mobile, AL, 36688, USA

    June E. Ayling

  2. Dept. of Biochemistry College of Medicine, University of South Alabama, Mobile, AL, 36688, USA

    M. Gopal Nair

  3. College of Medicine, Universily of South Alabama, Mobile, AL, 36688, USA

    Charles M. Baugh

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© 1993 Springer Science+Business Media New York

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Priest, D.G., Schmitz, J.C., Bunni, M.A. (1993). Folate Metabolites as Modulators of Antitumor Drug Activity. In: Ayling, J.E., Nair, M.G., Baugh, C.M. (eds) Chemistry and Biology of Pteridines and Folates. Advances in Experimental Medicine and Biology, vol 338. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-2960-6_143

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  • DOI: https://doi.org/10.1007/978-1-4615-2960-6_143

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-6287-6

  • Online ISBN: 978-1-4615-2960-6

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