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5-fluoro-2'-deoxyuridine-5'-monophosphate
- Development stage
- Preclinical
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
01
Overview
5-fluoro-2'-deoxyuridine-5'-monophosphate (FdUMP) is a nucleotide analog and the active metabolite of the chemotherapeutic agents 5-fluorouracil (5-FU) and floxuridine. It acts as a suicide inhibitor of thymidylate synthase, an enzyme essential for DNA synthesis. By forming a stable covalent complex with thymidylate synthase in the presence of its cofactor, FdUMP irreversibly inhibits the conversion of deoxyuridine monophosphate to deoxythymidine monophosphate, leading to depletion of thymidine nucleotides required for DNA replication and repair. This results in cell cycle arrest and apoptosis, particularly affecting rapidly dividing tumor cells. FdUMP is primarily used in cancer research and has been investigated as an antitumor agent due to its potent inhibition of DNA synthesis[4][6][1][5].
- Other names
- 5-fluoro-2'-deoxyuridine 5'-monophosphatefluorodeoxyuridylateFdUMP5-FdUMP
02
Targets
TS (Thymidylate synthase)
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