Activating Compound | Comment | Organism | Structure |
---|---|---|---|
CD45 | transmembrane receptor-like protein tyrosine phosphatase activating the SFK by dephosphorylation of the regulatory tyrosine residue | Homo sapiens | |
additional information | phosphorylation of the autoactivation tyrosine residue leads to activation of SFK, displacement of the PPII linker from the SH3 domain and the regulatory tyrosine residue from the SH2 domain, activation mechanisms, overview | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine | i.e. pp2, synthetic inhibitor, inhibits SFKs by binding competitively to the ATP-binding site | Homo sapiens | |
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine | i.e. pp1, synthetic inhibitor, inhibits SFKs by binding competitively to the ATP-binding site | Homo sapiens | |
caveolin | a non-catalytic inhibitor of SFKs, transient inhibition | Homo sapiens | |
Chk | i.e. Csk-homologous kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, Chk is also a 'non-catalytic inhibitor' binding directly to the SFK forming stable complexes and inhibiting it, mechanism, overview | Homo sapiens | |
Csk | i.e. C-terminal Src kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, mechanism, overview | Homo sapiens | |
additional information | SFKs are regulated involving autophosphorylation for activation and inhibition by diverse endogenous catalytic and non-catalytic inhibitors acting directly or via down-regulation of SFKs, recognition and mechanisms involving Csk and Chk, overview | Homo sapiens | |
protein tyrosine phosphatases | e.g. T-cell protein tyrosine phosphatase, catalytic inhibitor of SFKs dephosphorylating the autoactivation tyrosine residue of SFK which leads to inhibition of SFK | Homo sapiens | |
RACK1 | a non-catalytic inhibitor of SFKs, transient inhibition | Homo sapiens | |
WASP | a non-catalytic inhibitor of SFKs, e.g. c-Src, mechanism, transient inhibition | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [Src-family protein tyrosine kinase]-L-tyrosine | Homo sapiens | i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK | ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate | - |
? | |
additional information | Homo sapiens | Src-family protein tyrosine kinases are proto-oncogenic enzymes controlling mammalian cell growth and proliferation, the enzymes are regulated by activation through autophosphorylation of their kinase domain and by inhibition through phosphorylation of their regulatory tyrosine residue near the C-terminus, mechanism, overview, abberrant SFK activation contributes to cancer development | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | Src-family protein tyrosine kinases SFK are regulated by activation through autophosphorylation of their kinase domain and by inhibition through phosphorylation of their regulatory tyrosine residue near the C-terminus by e.g. Csk and Chk, recognition and phosphorylation mechanisms, overview | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Homo sapiens | - |
fibroblast | - |
Homo sapiens | - |
T-cell | - |
Homo sapiens | - |
T-lymphocyte | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a [protein]-L-tyrosine | - |
Homo sapiens | ADP + a [protein]-L-tyrosine phosphate | - |
? | |
ATP + [Src-family protein tyrosine kinase]-L-tyrosine | i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK | Homo sapiens | ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate | - |
? | |
additional information | Src-family protein tyrosine kinases are proto-oncogenic enzymes controlling mammalian cell growth and proliferation, the enzymes are regulated by activation through autophosphorylation of their kinase domain and by inhibition through phosphorylation of their regulatory tyrosine residue near the C-terminus, mechanism, overview, abberrant SFK activation contributes to cancer development | Homo sapiens | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | SFKs show active and inactive comformations depending on the tyrosine phosphorylation status, the inactive conformation is stabilized by intramolecular interactions, schematic modeling, overview | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
More | the Src kinase family consists of protein kinases c-Src, Fyn, Lck, Yes, Lyn, Hck, Fgr, Blk, and Yrk | Homo sapiens |
SFK | - |
Homo sapiens |
Src-family protein tyrosine kinase | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |