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Literature summary extracted from

  • Roy, A.C.; Lunn, F.A.; Bearne, S.L.
    Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids (2010), Bioorg. Med. Chem. Lett., 20, 141-144.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
6.3.4.2 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

EC Number Application Comment Organism
6.3.4.2 drug development CTP is a recognized target for the development of anticancer, antiviral, and antiprotozoal agents Escherichia coli

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.3.4.2 1,3,7,9-tetramethyluric
-
 Escherichia coli
6.3.4.2 1,3,7-trimethyluric acid
-
 Escherichia coli
6.3.4.2 1,3-dimethyluric acid pH-dependent inhibition, overview Escherichia coli
6.3.4.2 1,7-dimethyluric acid pH-dependent inhibition, overview Escherichia coli
6.3.4.2 1-methyluric acid
-
 Escherichia coli
6.3.4.2 3,7-dimethyluric acid
-
 Escherichia coli
6.3.4.2 adenine
-
 Escherichia coli
6.3.4.2 Caffeine
-
 Escherichia coli
6.3.4.2 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
6.3.4.2 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
6.3.4.2 paraxanthine pH-dependent inhibition, overview Escherichia coli
6.3.4.2 Theobromine
-
 Escherichia coli
6.3.4.2 theophylline pH-dependent inhibition, overview Escherichia coli
6.3.4.2 Uracil
-
 Escherichia coli
6.3.4.2 uracil-4-acetic acid
-
 Escherichia coli
6.3.4.2 uric acid pH-dependent inhibition, overview Escherichia coli
6.3.4.2 uridine
-
 Escherichia coli
6.3.4.2 xanthine pH-dependent inhibition, overview Escherichia coli

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
6.3.4.2 additional information
-
 additional information positive cooperativity for ATP and UTP Escherichia coli

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
6.3.4.2 UTP + ATP + NH3 Escherichia coli the enzyme is regulated in a complex fashion, overview CTP + ADP + phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
6.3.4.2 Escherichia coli
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.3.4.2 UTP + ATP + NH3 the enzyme is regulated in a complex fashion, overview Escherichia coli CTP + ADP + phosphate
-
 ?
6.3.4.2 UTP + ATP + NH3 NH3 from glutamine deamination or exogenous Escherichia coli CTP + ADP + phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.3.4.2 CTPS
-
 Escherichia coli

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
6.3.4.2 8 8.5 assay at Escherichia coli

Cofactor

EC Number Cofactor Comment Organism Structure
6.3.4.2 ATP
-
 Escherichia coli

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
6.3.4.2 additional information
-
 additional information inhibition kinetics. Multisite inhibition of CTPS-catalyzed NH3-dependent CTP formation by caffeine Escherichia coli

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.3.4.2 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
6.3.4.2 0.06
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli uric acid
6.3.4.2 0.063
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli 3,7-dimethyluric acid
6.3.4.2 0.067
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli 1,3,7-trimethyluric acid
6.3.4.2 0.07
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli 1,3,7-trimethyluric acid
6.3.4.2 0.072
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli 1,3-dimethyluric acid
6.3.4.2 0.079
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli 1,3,7,9-tetramethyluric
6.3.4.2 0.087
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli uric acid
6.3.4.2 0.088
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli 1,3-dimethyluric acid
6.3.4.2 0.09
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli 3,7-dimethyluric acid
6.3.4.2 0.096
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli 1-methyluric acid
6.3.4.2 0.101
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli 1-methyluric acid
6.3.4.2 0.113
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli 1,7-dimethyluric acid
6.3.4.2 0.119
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli 1,7-dimethyluric acid
6.3.4.2 0.121
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli 1,3,7,9-tetramethyluric
6.3.4.2 0.23
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli xanthine
6.3.4.2 0.37
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli xanthine
6.3.4.2 0.39
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli Caffeine
6.3.4.2 0.42
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli Theobromine
6.3.4.2 0.43
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli theophylline
6.3.4.2 0.44
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli paraxanthine
6.3.4.2 0.48
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli paraxanthine
6.3.4.2 0.51
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli Caffeine
6.3.4.2 0.55
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli theophylline
6.3.4.2 0.58
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli Theobromine
6.3.4.2 2.6
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli uracil-4-acetic acid
6.3.4.2 3.1
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli uridine
6.3.4.2 3.2
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli uracil-4-acetic acid
6.3.4.2 4.2
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli Uracil
6.3.4.2 4.6
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli uridine
6.3.4.2 4.7
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli Uracil
6.3.4.2 12.9
-
 pH 8.0, NH3-dependent CTP formation Escherichia coli adenine
6.3.4.2 15.8
-
 pH 8.0, Gln-dependent CTP formation Escherichia coli adenine

General Information

EC Number General Information Comment Organism
6.3.4.2 physiological function central role of CTP in the biosynthesis of nucleic acids, phospholipids, and sialic acid Escherichia coli