Any feedback?
Literature summary for 6.3.4.2 extracted from
- Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids (2010), Bioorg. Med. Chem. Lett., 20, 141-144.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| GTP | GTP acts a positive allosteric effector for Gln-dependent CTP formation. However, at concentrations exceeding 0.15 mM, GTP inhibits Gln-dependent CTP formation. Moreover, GTP is an inhibitor of NH3-dependent CTP formation at all concentrations | Escherichia coli |  |
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | CTP is a recognized target for the development of anticancer, antiviral, and antiprotozoal agents | Escherichia coli |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1,3,7,9-tetramethyluric | - |
Escherichia coli | |
| 1,3,7-trimethyluric acid | - |
Escherichia coli | |
| 1,3-dimethyluric acid | pH-dependent inhibition, overview | Escherichia coli | |
| 1,7-dimethyluric acid | pH-dependent inhibition, overview | Escherichia coli | |
| 1-methyluric acid | - |
Escherichia coli | |
| 3,7-dimethyluric acid | - |
Escherichia coli | |
| adenine | - |
Escherichia coli | |
| Caffeine | - |
Escherichia coli | |
| GTP | GTP acts a positive allosteric effector for Gln-dependent CTP formation. However, at concentrations exceeding 0.15 mM, GTP inhibits Gln-dependent CTP formation. Moreover, GTP is an inhibitor of NH3-dependent CTP formation at all concentrations | Escherichia coli | |
| additional information | inhibition by xanthine and derivatives, no inhibition by allantoin, an intact purine ring with anionic character favors inhibition. In general, methylation of the purine does not significantly affect inhibition | Escherichia coli | |
| paraxanthine | pH-dependent inhibition, overview | Escherichia coli | |
| Theobromine | - |
Escherichia coli | |
| theophylline | pH-dependent inhibition, overview | Escherichia coli | |
| Uracil | - |
Escherichia coli | |
| uracil-4-acetic acid | - |
Escherichia coli | |
| uric acid | pH-dependent inhibition, overview | Escherichia coli | |
| uridine | - |
Escherichia coli | |
| xanthine | pH-dependent inhibition, overview | Escherichia coli | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | positive cooperativity for ATP and UTP | Escherichia coli |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UTP + ATP + NH3 | Escherichia coli | the enzyme is regulated in a complex fashion, overview | CTP + ADP + phosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Escherichia coli | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UTP + ATP + NH3 | the enzyme is regulated in a complex fashion, overview | Escherichia coli | CTP + ADP + phosphate | - |
? | |
| UTP + ATP + NH3 | NH3 from glutamine deamination or exogenous | Escherichia coli | CTP + ADP + phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| CTPS | - |
Escherichia coli |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | 8.5 | assay at | Escherichia coli |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Escherichia coli | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics. Multisite inhibition of CTPS-catalyzed NH3-dependent CTP formation by caffeine | Escherichia coli |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| additional information | - |
xanthine and related compounds inhibit CTPS activity with IC50 = 0.16-0.58 mM. The presence of an 8-oxo function enhances the inhibition to IC50 = 0.060-0.121 mM. Raising the pH from 8.0 to 8.5 results in slightly increased inhibition of NH3-dependent CTP formation by the xanthines | Escherichia coli | additional information | |
| 0.06 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | uric acid | |
| 0.063 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | 3,7-dimethyluric acid | |
| 0.067 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | 1,3,7-trimethyluric acid | |
| 0.07 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | 1,3,7-trimethyluric acid | |
| 0.072 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | 1,3-dimethyluric acid | |
| 0.079 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | 1,3,7,9-tetramethyluric | |
| 0.087 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | uric acid | |
| 0.088 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | 1,3-dimethyluric acid | |
| 0.09 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | 3,7-dimethyluric acid | |
| 0.096 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | 1-methyluric acid | |
| 0.101 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | 1-methyluric acid | |
| 0.113 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | 1,7-dimethyluric acid | |
| 0.119 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | 1,7-dimethyluric acid | |
| 0.121 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | 1,3,7,9-tetramethyluric | |
| 0.23 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | xanthine | |
| 0.37 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | xanthine | |
| 0.39 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | Caffeine | |
| 0.42 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | Theobromine | |
| 0.43 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | theophylline | |
| 0.44 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | paraxanthine | |
| 0.48 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | paraxanthine | |
| 0.51 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | Caffeine | |
| 0.55 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | theophylline | |
| 0.58 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | Theobromine | |
| 2.6 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | uracil-4-acetic acid | |
| 3.1 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | uridine | |
| 3.2 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | uracil-4-acetic acid | |
| 4.2 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | Uracil | |
| 4.6 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | uridine | |
| 4.7 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | Uracil | |
| 12.9 | - |
pH 8.0, NH3-dependent CTP formation | Escherichia coli | adenine | |
| 15.8 | - |
pH 8.0, Gln-dependent CTP formation | Escherichia coli | adenine | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | central role of CTP in the biosynthesis of nucleic acids, phospholipids, and sialic acid | Escherichia coli |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
