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.
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 |
|