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Literature summary for 2.1.1.45 extracted from

  • Jason, T.L.; Berg, R.W.; Vincent, M.D.; Koropatnick, J.
    Antisense targeting of thymidylate synthase (TS) mRNA increases TS gene transcription and TS protein: effects on human tumor cell sensitivity to TS enzyme-inhibiting drugs (2007), Gene Expr., 13, 227-239.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.45

Application

Application Comment Organism
medicine thymidylate synthase is an important target for cancer chemotherapy Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information targeting of mRNA with antisense oligodeoxynucleotides, complementary to the translation start site, the coding region, and the 3' untranslated region. In response to treatment with translation start site-targeting antisense oligodeoxynucleotide 791, thymidylate synthase gene transcription in HeLa cells is increased by 70%. Increased thymidylate synthase gene transcription and nuclear thymidylate synthase RNA do not elevate levels of total cellular thymidylate synthase mRNA, but do increase thymidylate synthase protein activity by 35% and thymidylate synthase protein level by 150%. Increased thymidylate synthase protein activity and level do not alter proliferation rate or sensitivity to thymidylate synthase-targeting drugs Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5'-CGCGGTACGGACACCGCGCG-3' targets the TS mRNA translation start site TSS and increases the thymidylate synthase gene transcription in HeLa cell Homo sapiens
5-fluorodeoxyuridine 5-FUdR, TS-targeting chemotherapeutic agent Homo sapiens
5-fluorouracil 5-FU, TS-targeting chemotherapeutic agent Homo sapiens
pemetrexed TS-targeting chemotherapeutic agent Homo sapiens
raltitrexed TS-targeting chemotherapeutic agent 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 thymidylate synthase catalyses the only de novo pathway to produce thymidylate for DNA replication and repair 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
HeLa cell
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 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 thymidylate synthase catalyses the only de novo pathway to produce thymidylate for DNA replication and repair Homo sapiens 7,8-dihydrofolate + dTMP
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 ?