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Literature summary for 2.7.10.2 extracted from

  • Chong, Y.P.; Ia, K.K.; Mulhern, T.D.; Cheng, H.C.
    Endogenous and synthetic inhibitors of the Src-family protein tyrosine kinases (2005), Biochim. Biophys. Acta, 1754, 210-220.
    View publication on PubMed

Activating Compound

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

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 [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information
-
Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

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

Source Tissue Comment Organism Textmining
brain
-
Homo sapiens
-
fibroblast
-
Homo sapiens
-
T-cell
-
Homo sapiens
-
T-lymphocyte
-
Homo sapiens
-

Substrates and Products (Substrate)

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

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

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

Cofactor Comment Organism Structure
ATP
-
Homo sapiens