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Literature summary for 2.7.10.2 extracted from
- Activation mechanism and steady state kinetics of Brutons tyrosine kinase (2007), J. Biol. Chem., 282, 8768-8776.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| additional information | activation mechanism, autophosphorylation of Tyr551 causes a 10-fold increase in BTK activity | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| Y551F | site-directed mutagenesis, the mutant enzyme cannot be activated by autophosphorylation at Y551, and shows about 10fold reduced activation and activity compared to the wild-type enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ADP | competitive versus ATP, noncompetitive versus S1 peptide | Homo sapiens |  |
| staurosporine | competitive versus ATP, noncompetitive versus S1 peptide | Homo sapiens | |
| tyrophostin A25 | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | BTK steady state kinetics, kinetic mechanism, wild-type BTK and mutant Y551F | Homo sapiens | |
| 0.037 | - |
S1 peptide | BTK | Homo sapiens | |
| 0.084 | 0.09 | ATP | preactivated wild-type BTK | Homo sapiens | |
| 0.106 | - |
ATP | untreated wild-type BTK | Homo sapiens | |
| 0.124 | - |
ATP | preactivated BTK mutant Y551 | Homo sapiens | |
| 17.64 | - |
ATP | untreated BTK mutant Y551 | Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
| Mn2+ | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| phosphoprotein | BTK rapidly autophosphorylates at Tyr551 within its activation loop in vitro, phosphorylation of Tyr551 causes a 10fold increase in BTK activity | 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 + F peptide | i.e. biotin-Aca-AAAEEIFGEI-NH2 | Homo sapiens | ADP + phospho-L-tyrosinyl-F peptide | - |
? | |
| ATP + P1 peptide | i.e. biotin-Aca-AAAEEIpYGEI-NH2 | Homo sapiens | ADP + phospho-L-tyrosinyl-P1 peptide | - |
? | |
| ATP + S1 peptide | i.e. biotin-Aca-AAAEEIYGEI-NH2 | Homo sapiens | ADP + phospho-L-tyrosinyl-S1 peptide | - |
? | |
| additional information | BTK performs autophosphorylation | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Brutons tyrosine kinase | - |
Homo sapiens |
| Btk | - |
Homo sapiens |
| More | the enzyme belongs to the Tec nonreceptor tyrosine kinase family | 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 |
|---|---|---|---|
| 7.2 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | substrate inhibition kinetics and analysis | Homo sapiens |
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