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Literature summary for 2.7.10.2 extracted from

  • Lee, S.; Lin, X.; Nam, N.H.; Parang, K.; Sun, G.
    Determination of the substrate-docking site of protein tyrosine kinase C-terminal Src kinase (2003), Proc. Natl. Acad. Sci. USA, 100, 14707-14712.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.10.2

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant Csk in Escherichia coli strain DH5alpha Homo sapiens

Protein Variants

Protein Variants Comment Organism
D276A site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
E300A site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
F382A site-directed mutagenesis, reduced activity with substrate poly(Glu4-Tyr), and highly redcuced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
R281A/R283A site-directed mutagenesis, about 90% reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
S273A site-directed mutagenesis, reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
S280A site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
S280A/R281A/R283A/F381A site-directed mutagenesis, about 90% reduced activity with substrate [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
S284A site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens
S381A site-directed mutagenesis, reduced activity with substrates poly(Glu4-Tyr) and [kdSrc kinase]-L-tyrosine compared to the wild-type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information inhibition of the Src phosphorylation by peptides mimicking the substrate binding site, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0057
-
 [kdSrc kinase]-L-tyrosine pH 8.0, 30°C, recombinant wild-type enzyme Homo sapiens
0.0139
-
 [kdSrc kinase]-L-tyrosine pH 8.0, 30°C, recombinant mutant R281A/R283A Homo sapiens
0.0229
-
 [kdSrc kinase]-L-tyrosine pH 8.0, 30°C, recombinant mutant S280A/R281A/R283A/F381A Homo sapiens
0.095
-
 poly(Glu4-Tyr) pH 8.0, 30°C, recombinant wild-type enzyme Homo sapiens
0.274
-
 poly(Glu4-Tyr) pH 8.0, 30°C, recombinant mutant R281A/R283A Homo sapiens
0.322
-
 poly(Glu4-Tyr) pH 8.0, 30°C, recombinant mutant S280A/R281A/R283A/F381A Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
 Homo sapiens

Reaction

Reaction Comment Organism Reaction ID
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate substrate binding site involving residues R279, R281, and R283, more distant residues S280, F382, S273, and D276 are also important for activity Homo sapiens
a

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + poly(Glu4-Tyr)
-
 Homo sapiens ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
-
 ?
ATP + [kdSrc kinase]-L-tyrosine i.e. kinase-defective chicken Src mutant K295M Homo sapiens ADP + [kdSrc kinase]-L-tyrosine phosphate
-
 ?

Synonyms

Synonyms Comment Organism
C-terminal Src kinase
-
 Homo sapiens
Csk
-
 Homo sapiens
Protein tyrosine kinase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.11
-
 [kdSrc kinase]-L-tyrosine pH 8.0, 30°C, recombinant mutant R281A/R283A Homo sapiens
0.13
-
 [kdSrc kinase]-L-tyrosine pH 8.0, 30°C, recombinant mutant S280A/R281A/R283A/F381A Homo sapiens
0.9
-
 [kdSrc kinase]-L-tyrosine pH 8.0, 30°C, recombinant wild-type enzyme Homo sapiens
1.49
-
 poly(Glu4-Tyr) pH 8.0, 30°C, recombinant wild-type enzyme Homo sapiens
1.85
-
 poly(Glu4-Tyr) pH 8.0, 30°C, recombinant mutant S280A/R281A/R283A/F381A Homo sapiens
2.07
-
 poly(Glu4-Tyr) pH 8.0, 30°C, recombinant mutant R281A/R283A Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens