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Literature summary for 2.7.10.2 extracted from

  • Li, M.; Luraghi, P.; Amour, A.; Qian, X.D.; Carter, P.S.; Clark, C.J.; Deakin, A.; Denyer, J.; Hobbs, C.I.; Surby, M.; Patel, V.K.; Schaefer, E.M.
    Kinetic assay for characterization of spleen tyrosine kinase activity and inhibition with recombinant kinase and crude cell lysates (2009), Anal. Biochem., 384, 56-67.
    View publication on PubMed

Application

Application Comment Organism
medicine spleen tyrosine kinase is involved in the activation of cells implicated in allergic or autoimmune diseases and certain cancers, inhibitors may prove to be effective in treating diseases where Syk activity is increased or deregulated Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
full-length Syk is cloned into pFastBac HTb with an N-terminal 6-histidine tag and rTEV protease cleavage site, Syk protein is expressed in SF9 insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BAY61-3606
-
Homo sapiens
R112
-
Homo sapiens
R406
-
Homo sapiens
YM193306
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.014
-
ATP
-
Homo sapiens
0.057
-
EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ preactivation of the enzyme by incubation in the presence of 8.3 mM ATP and 16.6 mM MgCl2 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [protein]-L-tyrosine Homo sapiens
-
ADP + [protein]-L-tyrosine phosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
using a Ni-NTA Superflow and a Source 15Q column Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
Ramos cell
-
Homo sapiens
-

Storage Stability

Storage Stability Organism
-80°C, 20 mM MES buffer, pH 6.0, 200 mM NaCl, 10 mM betaMcEtOH, 10% glycerol, 1 mM benzamidine, 0.2 mM PMSF Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G Y7 Sox-based substrate, kinetic assay Homo sapiens ADP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G phosphate
-
?
ATP + [protein]-L-tyrosine
-
Homo sapiens ADP + [protein]-L-tyrosine phosphate
-
?

Synonyms

Synonyms Comment Organism
Spleen tyrosine kinase
-
Homo sapiens
Syk
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
55
-
ATP
-
Homo sapiens
396
-
EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP preactivation of the enzyme by incubation in the presence of 8.3 mM ATP and 16.6 mM MgCl2 Homo sapiens