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Literature summary for 2.1.1.45 extracted from

  • Okabe, T.; Okamoto, I.; Tsukioka, S.; Uchida, J.; Iwasa, T.; Yoshida, T.; Hatashita, E.; Yamada, Y.; Satoh, T.; Tamura, K.; Fukuoka, M.; Nakagawa, K.
    Synergistic antitumor effect of S-1 and the epidermal growth factor receptor inhibitor gefitinib in non-small cell lung cancer cell lines: role of gefitinib-induced down-regulation of thymidylate synthase (2008), Mol. Cancer Ther., 7, 599-606.
    View publication on PubMed

Application

Application Comment Organism
medicine the combination of the oral fluorouracil S-1 and the epidermal growth factor receptor-tyrosine kinase inhibitor gefitinib in shows a synergistic antiproliferative effect in vitro in all non-small cell lung cancer cell lines tested. Gefitinib inhibits the expression of the transcription factor E2F-1, resulting in the down-regulation of thymidylate synthase at the mRNA and protein levels Homo sapiens
medicine thymidylate synthase is a target in the treatment of cancer Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5-fluorouracil
-
Homo sapiens
gefitinib inhibits the expression of the transcription factor E2F-1, resulting in a down-regulation of thymidylate synthase at the mRNA and protein level; inhibits the expression of the transcription factor E2F-1, resulting in the down-regulation of thymidylate synthase at the mRNA and protein levels 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
-
7,8-dihydrofolate + dTMP
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens
-
patients with advanced non-small cell lung cancer
-

Source Tissue

Source Tissue Comment Organism Textmining
Ma-1 cell human NSCLC cell line Homo sapiens
-
Ma-25 cell human NSCLC cell line Homo sapiens
-
Ma-45 cell human NSCLC cell line Homo sapiens
-
Ma-53 cell human NSCLC cell line Homo sapiens
-
MiaPaCa-2 cell human NSCLC cell line Homo sapiens
-
NCI-H460 cell human NSCLC cell line Homo sapiens
-
non-small cell lung cancer cell line
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,10-methylenetetrahydrofolate + dUMP
-
Homo sapiens 7,8-dihydrofolate + dTMP
-
?

Synonyms

Synonyms Comment Organism
TS-DHFR
-
Homo sapiens