Relation Results

Summary

Name 2',2'-difluoro-2'-deoxyuridine
Synonyms
IUPAC 2'-deoxy-2',2'-difluorouridine
Formula C9H10F2N2O5
PRIMARY ID
(Read more)		 CHEBI:83486
Type chemical
Relations 1

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Type: Score: Layout: SPV 
0.82',2'-difluoro-2'-deoxyuridineTYMS

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+ 2',2'-difluoro-2'-deoxyuridinedown-regulates activity img/direct_inhibition.png chemical inhibition TYMS 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259351 Homo sapiens A2780/100 Cell
pmid sentence
2',2'-Difluoro-2'-deoxycytidine (dFdC, gemcitabine) is a cytidine analogue active against several solid tumor types, such as ovarian, pancreatic and non-small cell lung cancer. The compound has a complex mechanism of action. Because of the structural similarity of one metabolite of dFdC, dFdUMP, with the natural substrate for thymidylate synthase (TS) dUMP, we investigated whether dFdC and its deamination product 2',2'-difluoro-2'-deoxyuridine (dFdU) would inhibit TS. This study was performed using two solid tumor cell lines: the human ovarian carcinoma cell line A2780 and its dFdC-resistant variant AG6000. The specific TS inhibitor Raltitrexed (RTX) was included as a positive control. Using the in situ TS activity assay measuring the intracellular conversion of [5-(3)H]-2'-deoxyuridine or [5-(3)H]-2'-deoxycytidine to dTMP and tritiated water, it was observed that dFdC and dFdU inhibited TS.
Publications: 1 Organism: Homo Sapiens
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