BRENDA - Enzyme Database show

The sugar ring of the nucleoside is required for productive substrate positioning in the active site of human deoxycytidine kinase (dCK): implications for the development of dCK-activated acyclic guanine analogues

Hazra, S.; Konrad, M.; Lavie, A.; J. Med. Chem. 53, 5792-5800 (2010)

Data extracted from this reference:

Crystallization (Commentary)
EC Number
Crystallization
Organism
2.7.1.74
dCK in complex with acyclovir at the nucleoside phosphoryl acceptor site, and UDP at the phosphoryl donor site, hanging drop vapour diffusion method, 20 mg/ml protein with 5 mM UDP and 5 mM acyclovir is mixed with reservoir solution containing 0.90-1.5 M trisodium citrate dihydrate and 100 mM HEPES, pH 7.5, 12°C, X-ray diffraction structure determination and analysis at 2.1 A resolution, molecular replacement
Homo sapiens
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 + 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
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
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.7.1.74
Homo sapiens
P27707
-
-
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 + deoxyadenosine
-
722913
Homo sapiens
ADP + dAMP
-
-
-
?
2.7.1.74
ATP + deoxycytidine
-
722913
Homo sapiens
ADP + dCMP
-
-
-
?
2.7.1.74
ATP + deoxyguanosine
-
722913
Homo sapiens
ADP + dGMP
-
-
-
?
2.7.1.74
additional information
the human enzyme is not active with the acyclic guanine analogue acyclovir. Acyclovir binds at the dCK active site, but does so adopting a nonproductive conformation. Despite binding ACV, the enzyme remains in the open, inactive state, overview. dCK would phosphorylate acyclic guanine analogs if they can induce a similar rotation
722913
Homo sapiens
?
-
-
-
-
2.7.1.74
UTP + deoxyadenosine
-
722913
Homo sapiens
UDP + dAMP
-
-
-
?
2.7.1.74
UTP + deoxycytidine
-
722913
Homo sapiens
UDP + dCMP
-
-
-
?
2.7.1.74
UTP + deoxyguanosine
-
722913
Homo sapiens
UDP + dGMP
-
-
-
?
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
2.7.1.74
ATP
-
Homo sapiens
2.7.1.74
UTP
-
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
Crystallization (Commentary) (protein specific)
EC Number
Crystallization
Organism
2.7.1.74
dCK in complex with acyclovir at the nucleoside phosphoryl acceptor site, and UDP at the phosphoryl donor site, hanging drop vapour diffusion method, 20 mg/ml protein with 5 mM UDP and 5 mM acyclovir is mixed with reservoir solution containing 0.90-1.5 M trisodium citrate dihydrate and 100 mM HEPES, pH 7.5, 12°C, X-ray diffraction structure determination and analysis at 2.1 A resolution, molecular replacement
Homo sapiens
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 + 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
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
-
-
?
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 + deoxyadenosine
-
722913
Homo sapiens
ADP + dAMP
-
-
-
?
2.7.1.74
ATP + deoxycytidine
-
722913
Homo sapiens
ADP + dCMP
-
-
-
?
2.7.1.74
ATP + deoxyguanosine
-
722913
Homo sapiens
ADP + dGMP
-
-
-
?
2.7.1.74
additional information
the human enzyme is not active with the acyclic guanine analogue acyclovir. Acyclovir binds at the dCK active site, but does so adopting a nonproductive conformation. Despite binding ACV, the enzyme remains in the open, inactive state, overview. dCK would phosphorylate acyclic guanine analogs if they can induce a similar rotation
722913
Homo sapiens
?
-
-
-
-
2.7.1.74
UTP + deoxyadenosine
-
722913
Homo sapiens
UDP + dAMP
-
-
-
?
2.7.1.74
UTP + deoxycytidine
-
722913
Homo sapiens
UDP + dCMP
-
-
-
?
2.7.1.74
UTP + deoxyguanosine
-
722913
Homo sapiens
UDP + dGMP
-
-
-
?