BRENDA - Enzyme Database

Nucleotide binding to human UMP-CMP kinase using fluorescent derivatives - a screening based on affinity for the UMP-CMP binding site

Topalis, D.; Kumamoto, H.; Amaya Velasco, M.F.; Dugue, L.; Haouz, A.; Alexandre, J.A.; Gallois-Montbrun, S.; Alzari, P.M.; Pochet, S.; Agrofoglio, L.A.; Deville-Bonne, D.; FEBS J. 274, 3704-3714 (2007)

Data extracted from this reference:

Application
EC Number
Application
Commentary
Organism
2.7.4.14
medicine
screening of acyclic phosphonate analogs to find antimetabolites for antivirus and anticancer therapies
Homo sapiens
Cloned(Commentary)
EC Number
Commentary
Organism
2.7.4.14
overexpression in Escherichia coli, wild type and selenomethionine labelled protein
Homo sapiens
Crystallization (Commentary)
EC Number
Crystallization
Organism
2.7.4.14
of the selenomethionine labelled protein in complex with UMP, CMP, ADP, AMP-PCP, cidofovor and P1-(5’-adenosyl) P5-(5’-uridyl) pentaphosphate
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.4.14
5-Br-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-Cl-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-F-Phe-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-Phe-S-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-Phe-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
uracil vinylphosphonate
-
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.4.14
0.07
-
CMP
-
Homo sapiens
2.7.4.14
0.13
-
UMP
-
Homo sapiens
2.7.4.14
1
-
Cidofovir
-
Homo sapiens
2.7.4.14
1.1
-
dCMP
-
Homo sapiens
2.7.4.14
1.3
-
dUMP
-
Homo sapiens
Metals/Ions
EC Number
Metals/Ions
Commentary
Organism
Structure
2.7.4.14
Mg2+
-
Homo sapiens
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.7.4.14
Homo sapiens
P30085
-
-
Purification (Commentary)
EC Number
Commentary
Organism
2.7.4.14
of the recombinant protein
Homo sapiens
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.4.14
ATP + (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl) cytosine
Cidofovir
673598
Homo sapiens
ADP + (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl) cytosine
-
-
-
-
2.7.4.14
ATP + CMP
-
673598
Homo sapiens
ADP + CDP
-
-
-
?
2.7.4.14
ATP + dCMP
-
673598
Homo sapiens
ADP + dCDP
-
-
-
?
2.7.4.14
ATP + dUMP
no activity with CDP, dTMP, AMP, GMP
673598
Homo sapiens
ADP + dUDP
-
-
-
?
2.7.4.14
ATP + UMP
-
673598
Homo sapiens
ADP + UDP
-
-
-
?
Ki Value [mM]
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
2.7.4.14
0.016
-
5-Cl-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
0.017
-
5-Br-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
0.028
-
5-Phe-S-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
0.7
-
uracil vinylphosphonate
-
Homo sapiens
IC50 Value
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.7.4.14
0.03
-
-
Homo sapiens
5-Cl-uracil vinylphosphonate
2.7.4.14
0.035
-
-
Homo sapiens
5-Br-uracil vinylphosphonate
2.7.4.14
0.05
-
-
Homo sapiens
5-Phe-S-uracil vinylphosphonate
2.7.4.14
0.12
-
amplitude 50%
Homo sapiens
5-Phe-S-uracil vinylphosphonate
2.7.4.14
0.23
-
-
Homo sapiens
5-F-Phe-uracil vinylphosphonate
2.7.4.14
1.2
-
-
Homo sapiens
uracil vinylphosphonate
Application (protein specific)
EC Number
Application
Commentary
Organism
2.7.4.14
medicine
screening of acyclic phosphonate analogs to find antimetabolites for antivirus and anticancer therapies
Homo sapiens
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
2.7.4.14
overexpression in Escherichia coli, wild type and selenomethionine labelled protein
Homo sapiens
Crystallization (Commentary) (protein specific)
EC Number
Crystallization
Organism
2.7.4.14
of the selenomethionine labelled protein in complex with UMP, CMP, ADP, AMP-PCP, cidofovor and P1-(5’-adenosyl) P5-(5’-uridyl) pentaphosphate
Homo sapiens
IC50 Value (protein specific)
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.7.4.14
0.03
-
-
Homo sapiens
5-Cl-uracil vinylphosphonate
2.7.4.14
0.035
-
-
Homo sapiens
5-Br-uracil vinylphosphonate
2.7.4.14
0.05
-
-
Homo sapiens
5-Phe-S-uracil vinylphosphonate
2.7.4.14
0.12
-
amplitude 50%
Homo sapiens
5-Phe-S-uracil vinylphosphonate
2.7.4.14
0.23
-
-
Homo sapiens
5-F-Phe-uracil vinylphosphonate
2.7.4.14
1.2
-
-
Homo sapiens
uracil vinylphosphonate
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.4.14
5-Br-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-Cl-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-F-Phe-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-Phe-S-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
5-Phe-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
uracil vinylphosphonate
-
Homo sapiens
Ki Value [mM] (protein specific)
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
2.7.4.14
0.016
-
5-Cl-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
0.017
-
5-Br-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
0.028
-
5-Phe-S-uracil vinylphosphonate
-
Homo sapiens
2.7.4.14
0.7
-
uracil vinylphosphonate
-
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.4.14
0.07
-
CMP
-
Homo sapiens
2.7.4.14
0.13
-
UMP
-
Homo sapiens
2.7.4.14
1
-
Cidofovir
-
Homo sapiens
2.7.4.14
1.1
-
dCMP
-
Homo sapiens
2.7.4.14
1.3
-
dUMP
-
Homo sapiens
Metals/Ions (protein specific)
EC Number
Metals/Ions
Commentary
Organism
Structure
2.7.4.14
Mg2+
-
Homo sapiens
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
2.7.4.14
of the recombinant protein
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.4.14
ATP + (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl) cytosine
Cidofovir
673598
Homo sapiens
ADP + (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl) cytosine
-
-
-
-
2.7.4.14
ATP + CMP
-
673598
Homo sapiens
ADP + CDP
-
-
-
?
2.7.4.14
ATP + dCMP
-
673598
Homo sapiens
ADP + dCDP
-
-
-
?
2.7.4.14
ATP + dUMP
no activity with CDP, dTMP, AMP, GMP
673598
Homo sapiens
ADP + dUDP
-
-
-
?
2.7.4.14
ATP + UMP
-
673598
Homo sapiens
ADP + UDP
-
-
-
?