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Literature summary extracted from

  • Danenberg, P.V.
    Thymidylate synthetase - a target enzyme in cancer chemotherapy (1977), Biochim. Biophys. Acta, 473, 73-92.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.1.45 medicine
-
 Mus musculus
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
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 Lacticaseibacillus casei

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.45 (+)tetrahydropteroylglutamate
-
 Escherichia coli
2.1.1.45 2-amino-4-hydroxyquinazoline folic acid
-
 Enterococcus faecalis
2.1.1.45 2-amino-4-hydroxyquinazoline folic acid
-
 Lacticaseibacillus casei
2.1.1.45 2-amino-4-hydroxyquinazoline folic acid
-
 Mus musculus
2.1.1.45 2-amino-4-hydroxyquinazoline folic acid
-
 Streptococcus pneumoniae
2.1.1.45 3-beta-D-ribofuranosylmaleimide showdomycin Lacticaseibacillus casei
2.1.1.45 3-beta-D-ribofuranosylmaleimide 5'-phosphate showdomycin 5'-phosphate Lacticaseibacillus casei
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Enterococcus faecalis
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Escherichia coli
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Lacticaseibacillus casei
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Mus musculus
2.1.1.45 5-fluorouridine
-
 Homo sapiens
2.1.1.45 5-Formyl-2'-deoxyuridylic acid
-
 Escherichia coli
2.1.1.45 5-Formyl-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 5-Formyl-2'-deoxyuridylic acid
-
 Lacticaseibacillus casei
2.1.1.45 5-iodoacetamidomethyl-2'-deoxyuridine 5'-phosphate
-
 Mus musculus
2.1.1.45 5-Mercapto-2'-deoxyuridylic acid
-
 Escherichia coli
2.1.1.45 5-Mercapto-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 5-Mercapto-2'-deoxyuridylic acid possesses antitumor activity against Ehrlich ascites cells Mus musculus
2.1.1.45 5-trifluoromethyl-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 bromodeoxyuridine
-
 Homo sapiens
2.1.1.45 cytosine arabinoside
-
 Homo sapiens
2.1.1.45 diglutamate
-
 Escherichia coli
2.1.1.45 fluoroorotic acid
-
 Homo sapiens
2.1.1.45 glutamate
-
 Escherichia coli
2.1.1.45 iodoacetamide
-
 Lacticaseibacillus casei
2.1.1.45 Iododeoxyuridine
-
 Homo sapiens
2.1.1.45 N5-formyltetrahydropteroyloligoglutamate
-
 Escherichia coli
2.1.1.45 pteroylhexaglutamate
-
 Escherichia coli
2.1.1.45 pteroylhexaglutamate
-
 Lacticaseibacillus casei
2.1.1.45 tetrahydrohomofolate
-
 Escherichia coli

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 Streptococcus pneumoniae
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Mus musculus key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Escherichia coli key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Homo sapiens key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Enterococcus faecalis key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Lacticaseibacillus casei key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Escherichia coli biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism 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
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Enterococcus faecalis biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Escherichia coli B / ATCC 11303 key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Escherichia coli B / ATCC 11303 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 Enterococcus faecalis
-
-
-
2.1.1.45 Escherichia coli
-
-
-
2.1.1.45 Escherichia coli B / ATCC 11303
-
-
-
2.1.1.45 Homo sapiens
-
 human
-
2.1.1.45 Lacticaseibacillus casei
-
-
-
2.1.1.45 Mus musculus
-
 Ehrlich ascites carcinoma cells
-
2.1.1.45 Streptococcus pneumoniae
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.1.45
-
 Lacticaseibacillus casei

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.45 liver
-
 Mus musculus
-
2.1.1.45 liver
-
 Homo sapiens
-
2.1.1.45 neuroblastoma cell
-
 Mus musculus
-

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 0.17
-
-
 Enterococcus faecalis
2.1.1.45 0.27
-
-
 Enterococcus faecalis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.45 (-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
-
 Escherichia coli 7,8-dihydropteroylglutamate + thymidine phosphate
-
 ?
2.1.1.45 (-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
-
 Escherichia coli B / ATCC 11303 7,8-dihydropteroylglutamate + thymidine phosphate
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Mus musculus dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Escherichia coli dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Homo sapiens dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Enterococcus faecalis dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Streptococcus pneumoniae dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Streptococcus pneumoniae dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Lacticaseibacillus casei dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Mus musculus dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Escherichia coli dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Homo sapiens dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Enterococcus faecalis dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Lacticaseibacillus casei dihydrofolate + dTMP
-
 ?
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 Escherichia coli dihydrofolate + dTMP
-
 ?
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 5,10-methylenetetrahydrofolate + dUMP biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism Enterococcus faecalis dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Escherichia coli B / ATCC 11303 dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Escherichia coli B / ATCC 11303 dihydrofolate + dTMP
-
 ?
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 Escherichia coli B / ATCC 11303 dihydrofolate + dTMP
-
 ?
2.1.1.45 additional information
-
 Homo sapiens ?
-
 ?
2.1.1.45 additional information
-
 Enterococcus faecalis ?
-
 ?
2.1.1.45 additional information
-
 Streptococcus pneumoniae ?
-
 ?
2.1.1.45 additional information
-
 Lacticaseibacillus casei ?
-
 ?
2.1.1.45 additional information (+) forms are inhibitors Escherichia coli ?
-
 ?
2.1.1.45 additional information (+) forms are inhibitors Escherichia coli B / ATCC 11303 ?
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.45 0.00001
-
 5-Formyl-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 0.00001
-
 5-trifluoromethyl-2'-deoxyuridylic acid
-
 Homo sapiens
2.1.1.45 0.00004
-
 5-Mercapto-2'-deoxyuridylic acid
-
 Homo sapiens