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Literature summary for 2.1.1.45 extracted from
- Characteristics of thymidylate synthase purified from a human colon adenocarcinoma (1988), Arch. Biochem. Biophys., 260, 342-350.
Application
| Application | Comment | Organism |
|---|---|---|
| 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
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-fluorouracil | - |
Homo sapiens |  |
| pteroyldiglutamate | - |
Homo sapiens | |
| Pteroylheptaglutamate | - |
Homo sapiens | |
| pteroylhexaglutamate | - |
Homo sapiens | |
| pteroylmonoglutamate | - |
Homo sapiens | |
| pteroylpentaglutamate | - |
Homo sapiens | |
| pteroylpolyglutamate | - |
Homo sapiens | |
| pteroyltetraglutamate | - |
Homo sapiens | |
| Pteroyltriglutamate | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0035 | - |
[6R]methylenetetrahydropteroyltriglutamate | - |
Homo sapiens | |
| 0.0036 | - |
2'-deoxyuridylate | - |
Homo sapiens | |
| 0.0043 | - |
[6R]methylenetetrahydropteroylglutamate | - |
Homo sapiens | |
| 0.0043 | - |
[6R]methylenetetrahydropteroylheptaglutamate | - |
Homo sapiens | |
| 0.0065 | - |
[6R]methylenetetrahydropteroyldiglutamate | - |
Homo sapiens | |
| 0.0083 | - |
[6R]methylenetetrahydropteroylpentaglutamate | - |
Homo sapiens | |
| 0.0087 | - |
[6R]methylenetetrahydropteroylhexaglutamate | - |
Homo sapiens | |
| 0.0109 | - |
[6R]methylenetetrahydropteroyltetraglutamate | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 5,10-methylenetetrahydrofolate + dUMP | Sus scrofa | - |
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 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
human | - |
| Homo sapiens | - |
AML cells | - |
| Homo sapiens | - |
MCF-7 breast cancer cells | - |
| Sus scrofa | - |
pig | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| colon | adenocarcinoma | Homo sapiens | - |
| fetus | - |
Sus scrofa | - |
| liver | - |
Homo sapiens | - |
| liver | - |
Sus scrofa | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.0063 | - |
- |
Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 5,10-methylenetetrahydrofolate + dUMP | - |
Homo sapiens | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Sus scrofa | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Sus scrofa | dihydrofolate + dTMP | - |
r | |
| 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 | - |
? | |
| [6R]-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate | - |
Homo sapiens | ? | - |
r | |
| [6R]methylenetetrahydropteroyldiglutamate + dUMP | - |
Homo sapiens | 7,8-dihydropteroyldiglutamate + thymidine phosphate | - |
r | |
| [6R]methylenetetrahydropteroylheptaglutamate + dUMP | - |
Homo sapiens | 7,8-dihydropteroylheptaglutamate + thymidine phosphate | - |
r | |
| [6R]methylenetetrahydropteroylhexaglutamate + dUMP | - |
Homo sapiens | 7,8-dihydropteroylhexaglutamate + thymidine phosphate | - |
r | |
| [6R]methylenetetrahydropteroylpentaglutamate + dUMP | - |
Homo sapiens | 7,8-dihydropteroylpentaglutamate + thymidine phosphate | - |
r | |
| [6R]methylenetetrahydropteroyltetraglutamate + dUMP | - |
Homo sapiens | 7,8-dihydropteroyltetraglutamate + thymidine phosphate | - |
r | |
| [6R]methylenetetrahydropteroyltriglutamate + dUMP | - |
Homo sapiens | 7,8-dihydropteroyltriglutamate + thymidine phosphate | - |
r | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0006 | - |
pteroyltetraglutamate | - |
Homo sapiens | |
| 0.001 | - |
pteroylpentaglutamate | - |
Homo sapiens | |
| 0.002 | - |
pteroylhexaglutamate | - |
Homo sapiens | |
| 0.0034 | - |
Pteroyltriglutamate | - |
Homo sapiens | |
| 0.0034 | - |
Pteroylheptaglutamate | - |
Homo sapiens | |
| 0.0076 | - |
pteroylmonoglutamate | - |
Homo sapiens | |
| 0.0132 | - |
pteroyldiglutamate | - |
Homo sapiens | |
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