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Literature summary for 2.1.1.45 extracted from

  • Pillai, R.G.; Forster, M.; Perumal, M.; Mitchell, F.; Leyton, J.; Aibgirhio, F.I.; Golovko, O.; Jackman, A.L.; Aboagye, E.O.
    Imaging pharmacodynamics of the alpha-folate receptor-targeted thymidylate synthase inhibitor BGC 945 (2008), Cancer Res., 68, 3827-3834.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine pharmacological treatment of colorectal cancer Homo sapiens
medicine treatment with thymidylate synthase inhibitors BGC 945 and BGC 9331 results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd levels. BGC 9331 induces accumulation of [18F]-fluorothymidine in the intestine Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BGC 9331 treatment results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd levels. BGC 9331 induces accumulation of [18F]-fluorothymidine uptake in the intestine Homo sapiens
BGC 945 alpha-folate receptor targeted antifolate TS inhibitor; cyclopenta[g]quinazoline-based inhibitor. Treatment results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd 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
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
bone marrow
-
Homo sapiens
-
gut
-
Homo sapiens
-
intestine
-
Homo sapiens
-
KB cell
-
Homo sapiens
-
KB cell folate receptor-positive human epidermoid KB cell 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
-
?