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Literature summary extracted from

  • Radparvar, S.; Houghton, P.J.; Houghton, J.A.
    Characteristics of thymidylate synthase purified from a human colon adenocarcinoma (1988), Arch. Biochem. Biophys., 260, 342-350.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.1.45 medicine enzyme is believed to be the major site of the cytotoxic action of the cancer chemotherapeutic drug 5-fluorouracil, development of inhibitors as clinical useful drugs Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.45 5-fluorouracil
-
 Homo sapiens
2.1.1.45 pteroyldiglutamate
-
 Homo sapiens
2.1.1.45 Pteroylheptaglutamate
-
 Homo sapiens
2.1.1.45 pteroylhexaglutamate
-
 Homo sapiens
2.1.1.45 pteroylmonoglutamate
-
 Homo sapiens
2.1.1.45 pteroylpentaglutamate
-
 Homo sapiens
2.1.1.45 pteroylpolyglutamate
-
 Homo sapiens
2.1.1.45 pteroyltetraglutamate
-
 Homo sapiens
2.1.1.45 Pteroyltriglutamate
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.1.1.45 0.0035
-
 [6R]methylenetetrahydropteroyltriglutamate
-
 Homo sapiens
2.1.1.45 0.0036
-
 2'-deoxyuridylate
-
 Homo sapiens
2.1.1.45 0.0043
-
 [6R]methylenetetrahydropteroylglutamate
-
 Homo sapiens
2.1.1.45 0.0043
-
 [6R]methylenetetrahydropteroylheptaglutamate
-
 Homo sapiens
2.1.1.45 0.0065
-
 [6R]methylenetetrahydropteroyldiglutamate
-
 Homo sapiens
2.1.1.45 0.0083
-
 [6R]methylenetetrahydropteroylpentaglutamate
-
 Homo sapiens
2.1.1.45 0.0087
-
 [6R]methylenetetrahydropteroylhexaglutamate
-
 Homo sapiens
2.1.1.45 0.0109
-
 [6R]methylenetetrahydropteroyltetraglutamate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Sus scrofa
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Homo sapiens biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism dihydrofolate + dTMP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.45 Homo sapiens
-
 human
-
2.1.1.45 Homo sapiens
-
 AML cells
-
2.1.1.45 Homo sapiens
-
 MCF-7 breast cancer cells
-
2.1.1.45 Sus scrofa
-
 pig
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.1.45
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.45 colon adenocarcinoma Homo sapiens
-
2.1.1.45 fetus
-
 Sus scrofa
-
2.1.1.45 liver
-
 Homo sapiens
-
2.1.1.45 liver
-
 Sus scrofa
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.1.1.45 0.0063
-
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Homo sapiens dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Sus scrofa dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Sus scrofa dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism Homo sapiens dihydrofolate + dTMP
-
 ?
2.1.1.45 [6R]-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
-
 Homo sapiens ?
-
 r
2.1.1.45 [6R]methylenetetrahydropteroyldiglutamate + dUMP
-
 Homo sapiens 7,8-dihydropteroyldiglutamate + thymidine phosphate
-
 r
2.1.1.45 [6R]methylenetetrahydropteroylheptaglutamate + dUMP
-
 Homo sapiens 7,8-dihydropteroylheptaglutamate + thymidine phosphate
-
 r
2.1.1.45 [6R]methylenetetrahydropteroylhexaglutamate + dUMP
-
 Homo sapiens 7,8-dihydropteroylhexaglutamate + thymidine phosphate
-
 r
2.1.1.45 [6R]methylenetetrahydropteroylpentaglutamate + dUMP
-
 Homo sapiens 7,8-dihydropteroylpentaglutamate + thymidine phosphate
-
 r
2.1.1.45 [6R]methylenetetrahydropteroyltetraglutamate + dUMP
-
 Homo sapiens 7,8-dihydropteroyltetraglutamate + thymidine phosphate
-
 r
2.1.1.45 [6R]methylenetetrahydropteroyltriglutamate + dUMP
-
 Homo sapiens 7,8-dihydropteroyltriglutamate + thymidine phosphate
-
 r

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.45 0.0006
-
 pteroyltetraglutamate
-
 Homo sapiens
2.1.1.45 0.001
-
 pteroylpentaglutamate
-
 Homo sapiens
2.1.1.45 0.002
-
 pteroylhexaglutamate
-
 Homo sapiens
2.1.1.45 0.0034
-
 Pteroyltriglutamate
-
 Homo sapiens
2.1.1.45 0.0034
-
 Pteroylheptaglutamate
-
 Homo sapiens
2.1.1.45 0.0076
-
 pteroylmonoglutamate
-
 Homo sapiens
2.1.1.45 0.0132
-
 pteroyldiglutamate
-
 Homo sapiens