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Literature summary for 2.1.1.45 extracted from
- Kinetics of Plasmodium flaciparum thymidylate synthase: interactions with high-affinity metabolites of 5-fluoroorotate and D1694 (1996), Antimicrob. Agents Chemother., 40, 1628-1632.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | - |
Mus musculus |
| medicine | - |
Homo sapiens |
| medicine | - |
Crithidia fasciculata |
| medicine | - |
Plasmodium berghei |
| medicine | development of antimalarial drugs, selective chemoptherapy directed at malarial TS, inhibitors of pyrimidine biosynthesis shall be considered for malaria chemotherapy | Plasmodium falciparum |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| Escherichia coli cells carrying an expression plasmid with the malarial dihydrofolate reductase-thymidylate synthase | Plasmodium falciparum |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-fluoro-2'-deoxyuridylic acid | - |
Escherichia coli |  |
| 5-fluoro-2'-deoxyuridylic acid | - |
Homo sapiens | |
| 5-fluoro-2'-deoxyuridylic acid | - |
Leishmania major | |
| 5-fluoro-2'-deoxyuridylic acid | - |
Mus musculus | |
| 5-fluoro-2'-deoxyuridylic acid | - |
Plasmodium falciparum | |
| 5-Fluoroorotate | - |
Plasmodium falciparum | |
| 5-Fluoroorotate | - |
Plasmodium yoelii | |
| 5-fluorouracil | - |
Crithidia fasciculata | |
| 5-fluorouracil | - |
Escherichia coli | |
| 5-fluorouracil | - |
Homo sapiens | |
| 5-fluorouracil | - |
Plasmodium falciparum | |
| D1694 | - |
Mus musculus | |
| D1694 | - |
Plasmodium falciparum | |
| D1694 pentaglutamate | - |
Mus musculus | |
| D1694 pentaglutamate | - |
Plasmodium falciparum | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0013 | - |
2'-deoxyuridylate | native enzyme | Plasmodium falciparum | |
| 0.0018 | - |
2'-deoxyuridylate | - |
Homo sapiens | |
| 0.002 | - |
2'-deoxyuridylate | recombinant enzyme | Plasmodium falciparum | |
| 0.0034 | - |
2'-deoxyuridylate | - |
Escherichia coli | |
| 0.008 | - |
methylenetetrahydrofolate | - |
Homo sapiens | |
| 0.027 | - |
methylenetetrahydrofolate | - |
Mus musculus | |
| 0.03 | - |
5,10-methylenetetrahydrofolate | native enzyme | Plasmodium falciparum | |
| 0.031 | - |
methylenetetrahydrofolate | - |
Homo sapiens | |
| 0.039 | - |
5,10-methylenetetrahydrofolate | recombinant enzyme | Plasmodium falciparum | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 31000 | - |
2 * 31000, SDS-PAGE | Escherichia coli |
| 31000 | - |
2 * 31000, SDS-PAGE | Plasmodium falciparum |
| 71000 | - |
- |
Mus musculus |
| 71000 | - |
- |
Plasmodium falciparum |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 5,10-methylenetetrahydrofolate + dUMP | Mus musculus | - |
dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | Escherichia coli | - |
dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | Homo sapiens | - |
dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | Crithidia fasciculata | - |
dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | Plasmodium falciparum | - |
dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | Plasmodium berghei | - |
dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | Leishmania major | - |
dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | Plasmodium yoelii | - |
dihydrofolate + dTMP | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Crithidia fasciculata | - |
- |
- |
| Escherichia coli | - |
- |
- |
| Homo sapiens | - |
- |
- |
| Leishmania major | - |
formerly called Leishmania tropica | - |
| Mus musculus | - |
- |
- |
| Plasmodium berghei | - |
- |
- |
| Plasmodium falciparum | - |
- |
- |
| Plasmodium yoelii | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant enzyme, expressed in E. coli | Plasmodium falciparum |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.0255 | - |
- |
Plasmodium falciparum |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP | - |
Homo sapiens | 7,8-dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Mus musculus | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Mus musculus | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Escherichia coli | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Escherichia coli | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Homo sapiens | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Homo sapiens | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Crithidia fasciculata | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Crithidia fasciculata | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Plasmodium falciparum | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Plasmodium falciparum | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Plasmodium berghei | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Plasmodium berghei | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Leishmania major | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Leishmania major | dihydrofolate + dTMP | - |
r | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Plasmodium yoelii | dihydrofolate + dTMP | - |
? | |
| 5,10-methylenetetrahydrofolate + dUMP | - |
Plasmodium yoelii | dihydrofolate + dTMP | - |
r | |
| additional information | - |
Escherichia coli | ? | - |
? | |
| additional information | - |
Homo sapiens | ? | - |
? | |
| additional information | bifunctional enzyme dihydrofolate reductase-thymidylate synthase | Plasmodium falciparum | ? | - |
? | |
| additional information | bifunctional enzyme dihydrofolate reductase-thymidylate synthase | Leishmania major | ? | - |
? | |
| [6R,S]-5,10-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate | - |
Mus musculus | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| dimer | - |
Mus musculus |
| dimer | - |
Homo sapiens |
| dimer | - |
Plasmodium berghei |
| dimer | - |
Leishmania major |
| dimer | 2 * 31000, SDS-PAGE | Escherichia coli |
| dimer | 2 * 31000, SDS-PAGE | Plasmodium falciparum |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000006 | - |
D1694 | - |
Mus musculus | |
| 0.000001 | - |
D1694 pentaglutamate | - |
Mus musculus | |
| 0.0000015 | - |
D1694 pentaglutamate | - |
Plasmodium falciparum | |
| 0.0000017 | - |
5-fluoro-2'-deoxyuridylic acid | - |
Homo sapiens | |
| 0.000002 | - |
5-fluoro-2'-deoxyuridylic acid | - |
Plasmodium falciparum | |
| 0.0000028 | - |
D1694 | - |
Plasmodium falciparum | |
| 0.002 | - |
5-fluoro-2'-deoxyuridylic acid | - |
Plasmodium falciparum | |
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