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Literature summary for 3.5.4.1 extracted from

  • Wang, J.; Sklenak, S.; Liu, A.; Felczak, K.; Wu, Y.; Li, Y.; Yan, H.
    Role of glutamate 64 in the activation of the prodrug 5-fluorocytosine by yeast cytosine deaminase (2012), Biochemistry, 51, 475-486.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.4.1

Protein Variants

Protein Variants Comment Organism
E64A E64A mutation causes a decrease in kcat of 5 orders of magnitude and an increase in Km of 2 orders of magnitude, resulting in a decrease in kcat/Km of 8 orders of magnitude Saccharomyces cerevisiae
E64D the effect of E64D mutation are slightly milder than the E64A mutation Saccharomyces cerevisiae

Inhibitors

Inhibitors Comment Organism Structure
5-fluoro-1H-pyrimidin-2-one 19F NMR experiments show that binding of the inhibitor 5-fluoro-1H-pyrimidin-2-one (5FPy) to the wild-type yCD causes an upfield shift, indicating that the bound inhibitor is in the hydrated form, mimicking the transition state or the tetrahedral intermediate in the activation of 5FC. Binding of 5FPy to the E64A mutant enzyme causes a downfield shift, indicating that the bound 5FPy remains in an unhydrated form in the complex with the mutant enzyme Saccharomyces cerevisiae

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.16
-
 5-fluorocytosine wild-type, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae
8 9 5-fluorocytosine mutant E64A, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae
19
-
 5-fluorocytosine mutant E64D, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Saccharomyces cerevisiae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5-fluorocytosine + H2O
-
 Saccharomyces cerevisiae 5-fluorouracil + NH3
-
 ?

Synonyms

Synonyms Comment Organism
yCD
-
 Saccharomyces cerevisiae

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00013
-
 5-fluorocytosine mutant E64A, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae
0.005
-
 5-fluorocytosine mutant E64D, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae
17
-
 5-fluorocytosine wild-type, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Saccharomyces cerevisiae

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00086
-
 5-fluoro-1H-pyrimidin-2-one wild-type, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae
1.06
-
 5-fluoro-1H-pyrimidin-2-one mutant E64D, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.0000014
-
 5-fluorocytosine mutant E64A, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae
0.00026
-
 5-fluorocytosine mutant E64D, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae
106
-
 5-fluorocytosine wild-type, pH 7.5, temperature not specified in the publication Saccharomyces cerevisiae