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Literature summary for 6.3.4.2 extracted from
- Expression, purification, characterization, and in vivo targeting of trypanosome CTP synthetase for treatment of African sleeping sickness (2007), J. Biol. Chem., 282, 11858-11865.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | daily injection of acivicin in trypanosome-infected mice suppresses the infection up to one month without any significant loss of weight. Experiments with cultured bloodstream Trypanosoma brucei shows that acivicin is trypanocidal if present at 0.001 nM concentration for at least 4 d. Acivicin may qualify as a drug with desirable properties, i.e. cure within 7 d, according to the current Target Product Profiles of WHO and DNDi | Trypanosoma brucei |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| synthetase-His6-TEV protease site-tagged Trypanosoma brucei CTP synthetase is expressed in BL21(DE3) pLysS bacteria | Trypanosoma brucei |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| acivicin | irreversible inhibition by the glutamine analogue acivin. The acivicin inhibition of Trypanosoma brucei CTPS is more pronounced when the enzyme is preincubated with the drug in the presence of nucleotide substrates than in the absence of substrates | Trypanosoma brucei |  |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.07 | - |
ATP | - |
Trypanosoma brucei | |
| 0.07 | - |
GTP | - |
Trypanosoma brucei | |
| 0.16 | - |
UTP | - |
Trypanosoma brucei | |
| 0.26 | - |
L-glutamine | - |
Trypanosoma brucei | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | assay with 30 mM MgCl2 | Trypanosoma brucei | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Trypanosoma brucei | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| by using talon metal affinity resin, a glass Econo-Column and a Sephadex G-50 column. Proteolysis is performed at 23°C for 40 min. The protein solution is then loaded again on a Talon resin column but this time the flow-through, containing CTPS without His tag, is collected. Finally the protein is loaded onto a 0.2-ml SourceQ15 medium column. | Trypanosoma brucei |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
during the purification, the specific activity of the enzyme preparation increased 836fold and the total yield is 28% | Trypanosoma brucei |
| 0.00066 | - |
crude extract of protein | Trypanosoma brucei |
| 0.1119 | - |
1st Talon eluate | Trypanosoma brucei |
| 0.3986 | - |
TEV-cleaved 2nd Talon flow-through | Trypanosoma brucei |
| 0.5515 | - |
concentrated SourceQ flow-through | Trypanosoma brucei |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + UTP + Gln + H2O | - |
Trypanosoma brucei | ADP + CTP + Glu + phosphate | - |
? | |
| GTP + UTP + NH4+ | - |
Trypanosoma brucei | GDP + phosphate + CTP | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| CTP synthetase | - |
Trypanosoma brucei |
| CTPS | - |
Trypanosoma brucei |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Trypanosoma brucei |
pH Range
| pH Minimum | pH Maximum | Comment | Organism |
|---|---|---|---|
| 7.3 | - |
assay at | Trypanosoma brucei |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0023 | - |
acivicin | - |
Trypanosoma brucei | |
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