Protein Variants | Comment | Organism |
---|---|---|
D181A | substrate-trapping mutant | Homo sapiens |
D181A/Q262A | substrate-trapping mutant | Homo sapiens |
additional information | down-regulation of enzyme activity with small molecule inhibitors suppresses cell spreading and migration to fibronectin, increases Y527 phosphorylation in Src, and decreases phosphorylation of focal adhesion kinase, p130 Crk-associated substrate, and extracellular signal-regulated kinase 1/2 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide | - |
Homo sapiens | |
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide | dose-dependent increase in Y527 phosphorylation of Src | Homo sapiens | |
additional information | down-regulation of enzyme activity with small molecule inhibitors suppresses cell spreading and migration to fibronectin, increases Y527 phosphorylation in Src, and decreases phosphorylation of focal adhesion kinase, p130 Crk-associated substrate, and extracellular signal-regulated kinase 1/2 | Homo sapiens | |
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide | - |
Homo sapiens | |
N2-(2-((2-((N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalanyl)amino)ethyl)disulfanyl)ethyl)-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-argininamide | in presence of 5-50 nM, 11-35% decrease in cell spreading, 24% decrease in number of migratory cells, dose-dependent increase in Y527 phosphorylation of Src | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
phosphorylated p130 Crk-associated substrate + H2O | Homo sapiens | - |
p130 Crk-associated substrate + phosphate | - |
? | |
Y527-phosphorylated Src + H2O | Homo sapiens | - |
Src + phosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
recombinant enzyme, expression in Escherichia coli and L cell | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
phosphorylated p130 Crk-associated substrate + H2O | - |
Homo sapiens | p130 Crk-associated substrate + phosphate | - |
? | |
Y527-phosphorylated Src + H2O | - |
Homo sapiens | Src + phosphate | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000024 | - |
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide | - |
Homo sapiens | |
0.000026 | - |
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide | - |
Homo sapiens |