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Literature summary for 3.1.3.48 extracted from

  • Liang, F.; Lee, S.Y.; Liang, J.; Lawrence, D.S.; Zhang, Z.Y.
    The role of protein-tyrosine phosphatase 1B in integrin signaling (2005), J. Biol. Chem., 280, 24857-24863.
    View publication on PubMed

Protein Variants

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

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens
-
recombinant enzyme, expression in Escherichia coli and L cell
-

Substrates and Products (Substrate)

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 [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