BRENDA - Enzyme Database show

Phosphorylation of deoxycytidine kinase on Ser-74: impact on kinetic properties and nucleoside analog activation in cancer cells

Amsailale, R.; Van Den Neste, E.; Arts, A.; Starczewska, E.; Bontemps, F.; Smal, C.; Biochem. Pharmacol. 84, 43-51 (2012)

Data extracted from this reference:

Activating Compound
EC Number
Activating Compound
Commentary
Organism
Structure
2.7.1.74
aphidicolin
increases dCK activity via Ser74 phosphorylation, effect of aphidicolin treatment on dCK activity in leukemic cells with substrate deoxycytidine and cladribine and other substrates, overview
Homo sapiens
Application
EC Number
Application
Commentary
Organism
2.7.1.74
additional information
deoxycytidine kinase is a key enzyme in the activation of several therapeutic nucleoside analogues
Homo sapiens
Engineering
EC Number
Amino acid exchange
Commentary
Organism
2.7.1.74
S74E
site-directed mutagenesis, the mutation sensitizes the enzyme to feedback inhibition by dCTP, regardless of the phosphoryl donor. Mimicking Ser74 phosphorylation by a S74E mutation increases the enzyme activity toward pyrimidine analogues. The S74E mutation increased the kcat for cladribine by 8 or 3fold, depending on whether the phosphoryl donor was ATP or UTP, for clofarabine by about 2fold with both ATP and UTP, and for fludarabine by 2fold, but only with UTP
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.1.74
dCTP
a potent inhibitor of the enzyme when ATP is the phosphoryl donor, but a relatively weak inhibitor when the enzyme activity is measured with UTP as the phosphoryl donor. Inhibition is higher with respect to cladribine than deoxycytidine
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.1.74
0.00007
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.00009
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.00018
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.00027
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.00065
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0016
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0024
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.0087
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0155
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.0155
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.022
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.028
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0325
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.142
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.45
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.551
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
Localization
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
2.7.1.74
cytosol
-
Homo sapiens
5829
-
Metals/Ions
EC Number
Metals/Ions
Commentary
Organism
Structure
2.7.1.74
Mg2+
required
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.7.1.74
ATP + cladribine
Homo sapiens
-
ADP + cladribine 5'-phosphate
-
-
?
2.7.1.74
ATP + clofarabine
Homo sapiens
-
ADP + clofarabine 5'-phosphate
-
-
?
2.7.1.74
ATP + deoxyadenosine
Homo sapiens
-
ADP + dAMP
-
-
?
2.7.1.74
ATP + deoxycytidine
Homo sapiens
-
ADP + dCMP
-
-
?
2.7.1.74
ATP + deoxyguanosine
Homo sapiens
-
ADP + dGMP
-
-
?
2.7.1.74
ATP + fludarabine
Homo sapiens
-
ADP + fludarabine 5'-phosphate
-
-
?
2.7.1.74
UTP + cladribine
Homo sapiens
-
UDP + cladribine 5'-phosphate
-
-
?
2.7.1.74
UTP + clofarabine
Homo sapiens
-
UDP + clofarabine 5'-phosphate
-
-
?
2.7.1.74
UTP + deoxyadenosine
Homo sapiens
-
UDP + dAMP
-
-
?
2.7.1.74
UTP + deoxycytidine
Homo sapiens
-
UDP + dCMP
-
-
?
2.7.1.74
UTP + deoxyguanosine
Homo sapiens
-
UDP + dGMP
-
-
?
2.7.1.74
UTP + fludarabine
Homo sapiens
-
UDP + phospho-fludarabine
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.7.1.74
Homo sapiens
-
-
-
Posttranslational Modification
EC Number
Posttranslational Modification
Commentary
Organism
2.7.1.74
phosphoprotein
phosphorylation of deoxycytidine kinase on Ser74 increases the enzyme activity, increasing dCK activity via Ser74 phosphorylation, e.g. by aphidicolin, can enhance the intracellular activation of some nucleoside analogs, like gemcitabine, but not of cladribine or fludarabine, overview
Homo sapiens
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
2.7.1.74
chronic lymphocytic leukemia cell
-
Homo sapiens
-
2.7.1.74
HCT-116 cell
-
Homo sapiens
-
2.7.1.74
HT-29 cell
-
Homo sapiens
-
2.7.1.74
leukemia cell
-
Homo sapiens
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.1.74
ATP + cladribine
-
721556
Homo sapiens
ADP + cladribine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + clofarabine
-
721556
Homo sapiens
ADP + clofarabine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + deoxyadenosine
-
721556
Homo sapiens
ADP + dAMP
-
-
-
?
2.7.1.74
ATP + deoxycytidine
-
721556
Homo sapiens
ADP + dCMP
-
-
-
?
2.7.1.74
ATP + deoxyguanosine
-
721556
Homo sapiens
ADP + dGMP
-
-
-
?
2.7.1.74
ATP + fludarabine
-
721556
Homo sapiens
ADP + fludarabine 5'-phosphate
-
-
-
?
2.7.1.74
additional information
deoxycytidine kinase shows broad substrate specificity, catalyzing the phosphorylation of deoxycytidine, deoxyadenosine, and deoxyguanosine with ATP or UTP as phosphoryl donor
721556
Homo sapiens
?
-
-
-
-
2.7.1.74
UTP + cladribine
-
721556
Homo sapiens
UDP + cladribine 5'-phosphate
-
-
-
?
2.7.1.74
UTP + clofarabine
-
721556
Homo sapiens
UDP + clofarabine 5'-phosphate
-
-
-
?
2.7.1.74
UTP + deoxyadenosine
-
721556
Homo sapiens
UDP + dAMP
-
-
-
?
2.7.1.74
UTP + deoxycytidine
-
721556
Homo sapiens
UDP + dCMP
-
-
-
?
2.7.1.74
UTP + deoxyguanosine
-
721556
Homo sapiens
UDP + dGMP
-
-
-
?
2.7.1.74
UTP + fludarabine
-
721556
Homo sapiens
UDP + phospho-fludarabine
-
-
-
?
Temperature Optimum [°C]
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
2.7.1.74
37
-
assay at
Homo sapiens
Turnover Number [1/s]
EC Number
Turnover Number Minimum [1/s]
Turnover Number Maximum [1/s]
Substrate
Commentary
Organism
Structure
2.7.1.74
0.015
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.021
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0804
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.123
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.172
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.177
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.183
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.211
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.363
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.486
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.88
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
1.005
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
1.11
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
1.334
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
1.386
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
2.45
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
pH Optimum
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
2.7.1.74
7.6
-
assay at
Homo sapiens
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
2.7.1.74
ATP
-
Homo sapiens
2.7.1.74
UTP
-
Homo sapiens
Ki Value [mM]
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
2.7.1.74
0.0015
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates cladribine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.0029
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates deoxycytidine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.0058
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates cladribine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.027
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates cladribine and UTP, uncompetitive inhibition
Homo sapiens
2.7.1.74
0.03
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates deoxycytidine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.05
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates cladribine and UTP, uncompetitive inhibition
Homo sapiens
2.7.1.74
0.052
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates deoxycytidine and UTP, uncompetitive inhibition
Homo sapiens
2.7.1.74
0.398
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates deoxycytidine and UTP, uncompetitive inhibition
Homo sapiens
Activating Compound (protein specific)
EC Number
Activating Compound
Commentary
Organism
Structure
2.7.1.74
aphidicolin
increases dCK activity via Ser74 phosphorylation, effect of aphidicolin treatment on dCK activity in leukemic cells with substrate deoxycytidine and cladribine and other substrates, overview
Homo sapiens
Application (protein specific)
EC Number
Application
Commentary
Organism
2.7.1.74
additional information
deoxycytidine kinase is a key enzyme in the activation of several therapeutic nucleoside analogues
Homo sapiens
Cofactor (protein specific)
EC Number
Cofactor
Commentary
Organism
Structure
2.7.1.74
ATP
-
Homo sapiens
2.7.1.74
UTP
-
Homo sapiens
Engineering (protein specific)
EC Number
Amino acid exchange
Commentary
Organism
2.7.1.74
S74E
site-directed mutagenesis, the mutation sensitizes the enzyme to feedback inhibition by dCTP, regardless of the phosphoryl donor. Mimicking Ser74 phosphorylation by a S74E mutation increases the enzyme activity toward pyrimidine analogues. The S74E mutation increased the kcat for cladribine by 8 or 3fold, depending on whether the phosphoryl donor was ATP or UTP, for clofarabine by about 2fold with both ATP and UTP, and for fludarabine by 2fold, but only with UTP
Homo sapiens
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.1.74
dCTP
a potent inhibitor of the enzyme when ATP is the phosphoryl donor, but a relatively weak inhibitor when the enzyme activity is measured with UTP as the phosphoryl donor. Inhibition is higher with respect to cladribine than deoxycytidine
Homo sapiens
Ki Value [mM] (protein specific)
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
2.7.1.74
0.0015
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates cladribine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.0029
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates deoxycytidine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.0058
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates cladribine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.027
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates cladribine and UTP, uncompetitive inhibition
Homo sapiens
2.7.1.74
0.03
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates deoxycytidine and ATP, mixed inhibition
Homo sapiens
2.7.1.74
0.05
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates cladribine and UTP, uncompetitive inhibition
Homo sapiens
2.7.1.74
0.052
-
dCTP
pH 7.6, 37°C, enzyme mutant S74E, with substrates deoxycytidine and UTP, uncompetitive inhibition
Homo sapiens
2.7.1.74
0.398
-
dCTP
pH 7.6, 37°C, wild-type enzyme, with substrates deoxycytidine and UTP, uncompetitive inhibition
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.1.74
0.00007
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.00009
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.00018
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.00027
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.00065
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0016
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0024
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.0087
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0155
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.0155
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.022
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.028
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0325
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.142
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.45
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.551
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
Localization (protein specific)
EC Number
Localization
Commentary
Organism
GeneOntology No.
Textmining
2.7.1.74
cytosol
-
Homo sapiens
5829
-
Metals/Ions (protein specific)
EC Number
Metals/Ions
Commentary
Organism
Structure
2.7.1.74
Mg2+
required
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.7.1.74
ATP + cladribine
Homo sapiens
-
ADP + cladribine 5'-phosphate
-
-
?
2.7.1.74
ATP + clofarabine
Homo sapiens
-
ADP + clofarabine 5'-phosphate
-
-
?
2.7.1.74
ATP + deoxyadenosine
Homo sapiens
-
ADP + dAMP
-
-
?
2.7.1.74
ATP + deoxycytidine
Homo sapiens
-
ADP + dCMP
-
-
?
2.7.1.74
ATP + deoxyguanosine
Homo sapiens
-
ADP + dGMP
-
-
?
2.7.1.74
ATP + fludarabine
Homo sapiens
-
ADP + fludarabine 5'-phosphate
-
-
?
2.7.1.74
UTP + cladribine
Homo sapiens
-
UDP + cladribine 5'-phosphate
-
-
?
2.7.1.74
UTP + clofarabine
Homo sapiens
-
UDP + clofarabine 5'-phosphate
-
-
?
2.7.1.74
UTP + deoxyadenosine
Homo sapiens
-
UDP + dAMP
-
-
?
2.7.1.74
UTP + deoxycytidine
Homo sapiens
-
UDP + dCMP
-
-
?
2.7.1.74
UTP + deoxyguanosine
Homo sapiens
-
UDP + dGMP
-
-
?
2.7.1.74
UTP + fludarabine
Homo sapiens
-
UDP + phospho-fludarabine
-
-
?
Posttranslational Modification (protein specific)
EC Number
Posttranslational Modification
Commentary
Organism
2.7.1.74
phosphoprotein
phosphorylation of deoxycytidine kinase on Ser74 increases the enzyme activity, increasing dCK activity via Ser74 phosphorylation, e.g. by aphidicolin, can enhance the intracellular activation of some nucleoside analogs, like gemcitabine, but not of cladribine or fludarabine, overview
Homo sapiens
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
2.7.1.74
chronic lymphocytic leukemia cell
-
Homo sapiens
-
2.7.1.74
HCT-116 cell
-
Homo sapiens
-
2.7.1.74
HT-29 cell
-
Homo sapiens
-
2.7.1.74
leukemia cell
-
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.1.74
ATP + cladribine
-
721556
Homo sapiens
ADP + cladribine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + clofarabine
-
721556
Homo sapiens
ADP + clofarabine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + deoxyadenosine
-
721556
Homo sapiens
ADP + dAMP
-
-
-
?
2.7.1.74
ATP + deoxycytidine
-
721556
Homo sapiens
ADP + dCMP
-
-
-
?
2.7.1.74
ATP + deoxyguanosine
-
721556
Homo sapiens
ADP + dGMP
-
-
-
?
2.7.1.74
ATP + fludarabine
-
721556
Homo sapiens
ADP + fludarabine 5'-phosphate
-
-
-
?
2.7.1.74
additional information
deoxycytidine kinase shows broad substrate specificity, catalyzing the phosphorylation of deoxycytidine, deoxyadenosine, and deoxyguanosine with ATP or UTP as phosphoryl donor
721556
Homo sapiens
?
-
-
-
-
2.7.1.74
UTP + cladribine
-
721556
Homo sapiens
UDP + cladribine 5'-phosphate
-
-
-
?
2.7.1.74
UTP + clofarabine
-
721556
Homo sapiens
UDP + clofarabine 5'-phosphate
-
-
-
?
2.7.1.74
UTP + deoxyadenosine
-
721556
Homo sapiens
UDP + dAMP
-
-
-
?
2.7.1.74
UTP + deoxycytidine
-
721556
Homo sapiens
UDP + dCMP
-
-
-
?
2.7.1.74
UTP + deoxyguanosine
-
721556
Homo sapiens
UDP + dGMP
-
-
-
?
2.7.1.74
UTP + fludarabine
-
721556
Homo sapiens
UDP + phospho-fludarabine
-
-
-
?
Temperature Optimum [°C] (protein specific)
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
2.7.1.74
37
-
assay at
Homo sapiens
Turnover Number [1/s] (protein specific)
EC Number
Turnover Number Minimum [1/s]
Turnover Number Maximum [1/s]
Substrate
Commentary
Organism
Structure
2.7.1.74
0.015
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.021
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.0804
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.123
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.172
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
0.177
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.183
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
0.211
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.363
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
0.486
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
0.88
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
1.005
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
1.11
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
1.334
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
1.386
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
2.45
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
pH Optimum (protein specific)
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
2.7.1.74
7.6
-
assay at
Homo sapiens
General Information
EC Number
General Information
Commentary
Organism
2.7.1.74
additional information
deoxycytidine kinase is a key enzyme in the activation of several therapeutic nucleoside analogues
Homo sapiens
General Information (protein specific)
EC Number
General Information
Commentary
Organism
2.7.1.74
additional information
deoxycytidine kinase is a key enzyme in the activation of several therapeutic nucleoside analogues
Homo sapiens
KCat/KM [mM/s]
EC Number
kcat/KM Value [1/mMs-1]
kcat/KM Value Maximum [1/mMs-1]
Substrate
Commentary
Organism
Structure
2.7.1.74
1.8
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
2.6
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
3
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
6.4
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
50.1
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
56.3
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
57.6
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
74.3
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
76.8
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
90.2
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
130
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
136
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
236
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
257
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
676
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
745
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
KCat/KM [mM/s] (protein specific)
EC Number
KCat/KM Value [1/mMs-1]
KCat/KM Value Maximum [1/mMs-1]
Substrate
Commentary
Organism
Structure
2.7.1.74
1.8
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
2.6
-
fludarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
3
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
6.4
-
fludarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
50.1
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
56.3
-
clofarabine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
57.6
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
74.3
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
76.8
-
clofarabine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
90.2
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
130
-
cladribine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
136
-
cladribine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens
2.7.1.74
236
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate ATP
Homo sapiens
2.7.1.74
257
-
deoxycytidine
pH 7.6, 37°C, wild-type enzyme, with co-substrate UTP
Homo sapiens
2.7.1.74
676
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate ATP
Homo sapiens
2.7.1.74
745
-
deoxycytidine
pH 7.6, 37°C, enzyme mutant S74E, with co-substrate UTP
Homo sapiens