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Literature summary for 2.1.1.45 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

Application Comment Organism
medicine
-
Mus musculus
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
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

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5,10-methylenetetrahydrofolate + dUMP Streptococcus pneumoniae
-
dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP Mus musculus key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP Escherichia coli key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP Homo sapiens key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP Enterococcus faecalis key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP Lacticaseibacillus casei key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
?
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
-
?
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
-
?
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
-
?
5,10-methylenetetrahydrofolate + dUMP Escherichia coli B / ATCC 11303 key function in DNA synthesis, repair and cell division dihydrofolate + dTMP
-
?
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

Organism UniProt Comment Textmining
Enterococcus faecalis
-
-
-
Escherichia coli
-
-
-
Escherichia coli B / ATCC 11303
-
-
-
Homo sapiens
-
human
-
Lacticaseibacillus casei
-
-
-
Mus musculus
-
Ehrlich ascites carcinoma cells
-
Streptococcus pneumoniae
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Lacticaseibacillus casei

Source Tissue

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

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.17
-
-
Enterococcus faecalis
0.27
-
-
Enterococcus faecalis

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
-
Escherichia coli 7,8-dihydropteroylglutamate + thymidine phosphate
-
?
(-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
-
Escherichia coli B / ATCC 11303 7,8-dihydropteroylglutamate + thymidine phosphate
-
?
5,10-methylenetetrahydrofolate + dUMP
-
Mus musculus dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP
-
Escherichia coli dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP
-
Homo sapiens dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP
-
Enterococcus faecalis dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP
-
Streptococcus pneumoniae dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP
-
Streptococcus pneumoniae dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP
-
Lacticaseibacillus casei dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Mus musculus dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Escherichia coli dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Homo sapiens dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Enterococcus faecalis dihydrofolate + dTMP
-
?
5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Lacticaseibacillus casei dihydrofolate + dTMP
-
?
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
-
?
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
-
?
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
-
?
5,10-methylenetetrahydrofolate + dUMP
-
Escherichia coli B / ATCC 11303 dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP key function in DNA synthesis, repair and cell division Escherichia coli B / ATCC 11303 dihydrofolate + dTMP
-
?
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
-
?
additional information
-
Homo sapiens ?
-
?
additional information
-
Enterococcus faecalis ?
-
?
additional information
-
Streptococcus pneumoniae ?
-
?
additional information
-
Lacticaseibacillus casei ?
-
?
additional information (+) forms are inhibitors Escherichia coli ?
-
?
additional information (+) forms are inhibitors Escherichia coli B / ATCC 11303 ?
-
?

Ki Value [mM]

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