BRENDA - Enzyme Database show

Kinetic studies on 2',2'-difluorodeoxycytidine (gemcitabine) with purified human deoxycytidine kinase and cytidine deaminase

Bouffard, D.Y.; Laliberte, J.; Momparler, R.L.; Biochem. Pharmacol. 45, 1857-1861 (1993)

Data extracted from this reference:

Application
EC Number
Application
Commentary
Organism
3.5.4.5
medicine
enzyme limits the effectiveness of the antineoplastic agent cytosine arabinoside or aracytidine in the treatment of acute myeloblastic leukemias, chemotherapeutic use of the inhibitor THU to protect antileukemic agents from deaminase attack, inhibitors of cytidine deaminase prolongs the plasma halflife of antitumor or antiviral drugs
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
3.5.4.5
3,4,5,6-Tetrahydrouridine
-
Homo sapiens
3.5.4.5
diazepinone riboside
-
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
3.5.4.5
0.0463
-
deoxycytidine
-
Homo sapiens
3.5.4.5
0.0957
-
2',2'-difluorodeoxycytidine
-
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.5.4.5
cytidine + H2O
Homo sapiens
-
uridine + NH3
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
3.5.4.5
Homo sapiens
-
human
-
Purification (Commentary)
EC Number
Commentary
Organism
3.5.4.5
-
Homo sapiens
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
3.5.4.5
liver
-
Homo sapiens
-
3.5.4.5
placenta
-
Homo sapiens
-
3.5.4.5
spleen
-
Homo sapiens
-
Specific Activity [micromol/min/mg]
EC Number
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
3.5.4.5
0.011
-
-
Homo sapiens
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.4.5
2',2'-difluorodeoxycytidine + H2O
gemcitabine, antimetabolite of deoxycytidine, active against solid tumors and leukemic cell lines, deamination by the enzyme results in loss of pharmacologic activity
209663
Homo sapiens
2',2'-difluorodeoxyuridine + NH3
-
209663
Homo sapiens
?
3.5.4.5
cytidine + H2O
-
209663
Homo sapiens
uridine + NH3
-
-
-
?
Application (protein specific)
EC Number
Application
Commentary
Organism
3.5.4.5
medicine
enzyme limits the effectiveness of the antineoplastic agent cytosine arabinoside or aracytidine in the treatment of acute myeloblastic leukemias, chemotherapeutic use of the inhibitor THU to protect antileukemic agents from deaminase attack, inhibitors of cytidine deaminase prolongs the plasma halflife of antitumor or antiviral drugs
Homo sapiens
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
3.5.4.5
3,4,5,6-Tetrahydrouridine
-
Homo sapiens
3.5.4.5
diazepinone riboside
-
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
3.5.4.5
0.0463
-
deoxycytidine
-
Homo sapiens
3.5.4.5
0.0957
-
2',2'-difluorodeoxycytidine
-
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
3.5.4.5
cytidine + H2O
Homo sapiens
-
uridine + NH3
-
-
?
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
3.5.4.5
-
Homo sapiens
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
3.5.4.5
liver
-
Homo sapiens
-
3.5.4.5
placenta
-
Homo sapiens
-
3.5.4.5
spleen
-
Homo sapiens
-
Specific Activity [micromol/min/mg] (protein specific)
EC Number
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
3.5.4.5
0.011
-
-
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.4.5
2',2'-difluorodeoxycytidine + H2O
gemcitabine, antimetabolite of deoxycytidine, active against solid tumors and leukemic cell lines, deamination by the enzyme results in loss of pharmacologic activity
209663
Homo sapiens
2',2'-difluorodeoxyuridine + NH3
-
209663
Homo sapiens
?
3.5.4.5
cytidine + H2O
-
209663
Homo sapiens
uridine + NH3
-
-
-
?