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Literature summary for 2.7.10.2 extracted from

  • Chong, Y.P.; Chan, A.S.; Chan, K.C.; Williamson, N.A.; Lerner, E.C.; Smithgall, T.E.; Bjorge, J.D.; Fujita, D.J.; Purcell, A.W.; Scholz, G.; Mulhern, T.D.; Cheng, H.C.
    C-terminal Src kinase-homologous kinase (CHK), a unique inhibitor inactivating multiple active conformations of Src family tyrosine kinases (2006), J. Biol. Chem., 281, 32988-32999.
    View publication on PubMed
Search for more literature for 2.7.10.2

Activating Compound

Activating Compound Comment Organism Structure
additional information constitutive SFK activation is associated with tumorigenesis, Hck and Lyn perform autophosphorylation for activation Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of Hck mutant K267M and Lyn mutant K274M in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system Homo sapiens

Protein Variants

Protein Variants Comment Organism
K267M a Hck mutant, the inability of HckK267M to undergo autophosphorylation promotes its phosphorylation at YT by CSK to a higher extent than that of wild type Hck Homo sapiens
K274M Lyn mutant, Lyn K274M does not form a stable protein complex with CHK, whereas its unphosphorylated counterpart does Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
C-terminal Src kinase i.e. CSK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview Homo sapiens
CSK-homologous kinase i.e. CHK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, a second non-catalytic inhibitory mechanism involves tight binding of CHK to the enzyme's SFKs. The binding alone is sufficient to inhibit SFKs inhibition, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens
Mn2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + Src family kinase Homo sapiens substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview ?
-
 ?
additional information Homo sapiens the Src family of protein kinases mediates mitogenic signal transduction, and constitutive activation of the enzymes is associated with tumorigenesis ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein Hck and Lyn perform autophosphorylation for activation Homo sapiens

Purification (Commentary)

Purification (Comment) Organism
recombinant Lyn mutant K274M from Spodoptera frugiperda Sf9 cells by anion exchange and hydroxyapatite chromatography Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + cdc2(6-20) peptide i.e. KVEKIGEGTYGVVYK, substrate of Src family kinases Homo sapiens ?
-
 ?
ATP + Src family kinase substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview Homo sapiens ?
-
 ?
additional information the Src family of protein kinases mediates mitogenic signal transduction, and constitutive activation of the enzymes is associated with tumorigenesis Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
C-terminal Src kinase
-
 Homo sapiens
CHK
-
 Homo sapiens
Csk
-
 Homo sapiens
CSK-homologous kinase
-
 Homo sapiens
Lyn
-
 Homo sapiens
SFK
-
 Homo sapiens
Src family kinase
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
 assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens