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BIOLOGICAL INFO
Solubility:
DMSO: 49mg/mL; H2O: 49mg/mL; EtOH: 10mg/mL
Application(s):
Thymidylate synthetase inhibitor; DNA synthesis inhibitor
Form:
Free Base
REVIEW Floxuridine is rapidly catabolized to 5-fluorouracil, which is the active form of the drug. The primary effect is interference with DNA synthesis and to a lesser extent, inhibition of RNA formation through the drug''s incorporation into RNA, thus leading to the production of fraudulent RNA. Fluorouracil also inhibits uracil riboside phophorylase, which prevents the utilization of preformed uracil in RNA synthesis. As well, the monophosphate of floxuridine, 5-fluoro-2''-deoxyuridine-5''-phosphate (FUDR-MP) inhibits the enzyme thymidylate synthetase. This leads to the inhibition of methylation of deoxyuridylic acid to thymidylic acid, thus interfering with DNA synthesis.
REFERENCES
[1]
Tsume Y, Amidon GL (2012). The feasibility of enzyme targeted activation for amino acid/dipeptide monoester prodrugs of floxuridine; cathepsin D as a potential targeted enzyme. Molecules. 17(4):3672-89. PMID 22450679.
[2]
Rivero CW, Britos CN, Lozano ME, Sinisterra JV, Trelles JA (2012). Green biosynthesis of floxuridine by immobilized microorganisms. FEMS Microbiol Lett. 331(1):31-6. PMID 22428623.
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