Target intelligence / Profile preview

DNA Synthesis (via 5-Fluorouracil)

Molecular classification
Enzymatic pathway/process
01

Overview

Targeting DNA synthesis via thymidylate synthase inhibition using 5-fluorouracil exploits cancer cells' high demand for nucleotide precursors during rapid proliferation. The cytotoxic effect arises from both direct inhibition of thymidine production needed for new DNA strands and disruption caused by abnormal incorporation into both nuclear material and especially ribosomal RNA—a dual mechanism now recognized as central to its anticancer efficacy.

Other names
Thymidylate synthase inhibitionFluoropyrimidine antimetabolite therapy5-FU chemotherapydTTP depletion
02

Mechanism of action

Irreversible inhibition of thymidylate synthase (TS) by FdUMP; misincorporation of FdUTP into DNA; incorporation of FUTP into RNA.

03

Biological functions

DNA replicationCell proliferationCell cycleRNA processingTranslation
04

Disease associations

Cancer
05

Safety considerations

MyelosuppressionMucositisHand-foot syndromeNeurotoxicityCardiotoxicityDihydropyrimidine dehydrogenase (DPD) deficiency
06

Interacting drugs

5-Fluorouracil

1 more in the full profile.

07

Biomarkers

Dihydropyrimidine dehydrogenase (DPD) activity/expression (predicts toxicity)Thymidylate synthase (TS) expression (predicts response)

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