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Literature summary for 2.1.1.45 extracted from

  • Waldman, B.C.; Wang, Y.; Kilaru, K.; Yang, Z.; Bhasin, A.; Wyatt, M.D.; Waldman, A.S.
    Induction of intrachromosomal homologous recombination in human cells by raltitrexed, an inhibitor of thymidylate synthase (2008), DNA Repair, 7, 1624-1635.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine the use of the TS inhibitor RTX in the treatment of colorectal cancer has been approved in Europe, Canada, Australia and Japan Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
raltitrexed RTX, a folate analog that is a specific inhibitor of TS; treatment can stimulate accurate recombination events in human cells. Gene conversions not associated with crossovers are specifically enhanced severalfold. Recombination events provoked by a double-strand break are not impacted by treatment with raltitrexed, nor is error-prone double-strand break repair via nonhomologous end-joining Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5,10-methylenetetrahydrofolate + dUMP Homo sapiens during TS inhibition, TMP levels decrease with a subsequent increase in dUTP 7,8-dihydrofolate + dTMP
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Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
GM00637 cell normal human fibroblast cell line immortalized by SV40 Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,10-methylenetetrahydrofolate + dUMP
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Homo sapiens 7,8-dihydrofolate + dTMP
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5,10-methylenetetrahydrofolate + dUMP during TS inhibition, TMP levels decrease with a subsequent increase in dUTP Homo sapiens 7,8-dihydrofolate + dTMP
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?