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. 2021 Jul 15;11:688377. doi: 10.3389/fonc.2021.688377

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Copyright © 2021 Principe, Underwood, Korc, Trevino, Munshi and Rana

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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5-Fluorouracil mechanism of action. 5-Fluorouracil (5-FU) enters target cells in a similar manner to uracil, mainly by facilitated transport. Like Gemcitabine, 5-Fluorouracil (5-FU) is modified extensively in the cytoplasm. This includes conversion to Fluorodeoxyuridine monophosphate (FdUMP) by Thymidine Phosphorylase, inhibiting Thymidylate Synthase and potentiated by the addition of Leucovorin. In a parallel mechanism, 5-FU can be further modified to Fluorodeoxyuridine triphosphate, which subsequently inhibits RNA Polymerase.