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Literature summary extracted from

  • Mol, C.D.; Dougan, D.R.; Schneider, T.R.; Skene, R.J.; Kraus, M.L.; Scheibe, D.N.; Snell, G.P.; Zou, H.; Sang, B.C.; Wilson, K.P.
    Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase (2004), J. Biol. Chem., 279, 31655-31663.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.10.1 expression of a His-tagged enzyme fragment comprising residues 544-693 and 754-935, lacking the kinase insertion domain KID, in Spodoptera frugiperda cells Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.10.1 purified recombinant His-tagged enzyme fragment, activated or autoinhibited, comprising residues 544-693 and 754-935, sitting drop vapour diffusion method, 0.005 ml active protein solution, containing 6 mg/ml protein 250 mM NaCl, MgCl2, and ATP, are mixed with 0.005 ml reservoir solution containing 18% polyethylene glycol 8000, 0.1 M MES, pH 7.1, 20°C, 50 nl autoinhibited protein solution is mixed with 50 nl reservoir solution containing 13% PEG 8000, 0.1 M HEPES, pH 7.0, co-crystallization with inhibitor STI-571 50 nl inhibitor solution and 50 nl reservoir solution containing 2 M phosphate, 0.1 M Tris, pH 8.5 are utilized, X-ray diffraction structure determination and analysis at about 1.38 A Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.1 additional information enzyme performs autoinhibition via its juxtamembrane domain, structure and mechanism, overview Homo sapiens
2.7.10.1 STI-571
-
Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.10.1 membrane enzyme contains a juxtamembrane domain acting as a pseudosubstrate responsible for autoinhibition of the enzyme, structure overview Homo sapiens 16020
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.10.1 Mg2+ coordinates with Asp810 within the c-Kit DFG motif, overview Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.10.1 Homo sapiens P10721 juxtamembrane domain and catalytic domains of c-Kit receptor protein-tyrosine kinase, residues 544-935
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.10.1 recombinant His-tagged enzyme fragment comprising residues 544-693 and 754-935 by nickel chelate affinity chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.10.1 ATP + a [protein]-L-tyrosine substrate binding and active structure Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.10.1 c-Kit receptor protein-tyrosine kinase
-
Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.10.1 20
-
assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.10.1 ATP
-
Homo sapiens