Inhibitors | Comment | Organism | Structure |
---|---|---|---|
bis(2-ethyl-maltolato)oxidovanadium(IV) | noncompetitive inhibition of hydrolysis of 4-nitrophenyl phosphate and of phosphorylated undecapeptide substrate EGFR988-998 in the presence of bis(2-ethyl-maltolato)oxidovanadium(IV) | Homo sapiens | |
bis(2-methyl-maltolato)oxidovanadium(IV) | - |
Homo sapiens | |
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV) | - |
Homo sapiens | |
bis(acetylacetonato)oxidovanadium(IV) | acts as an uncompetitive inhibitor of PTP1B with DADEpYLIPQQG as the substrate, but this VO2+-chelate exhibits only apparent competitive inhibition of 4-nitrophenyl phosphate hydrolysis when catalyzed by PTP1B, differing from that observed in the hydrolysis of the phosphotyrosine-containing undecapeptide DADEpYLIPQQG mimicking residues 988-998 of the epidermal growth factor receptor (EGFR). Addition of 4-nitrophenyl phosphate after addition of saturating amounts of bis(acetylacetonato)oxidovanadium(IV) to PTP1B causes complete loss of catalytic activity | Homo sapiens | |
additional information | inhibition of protein tyrosine phosphatase-1B by vanadyl (VO2+) chelates, competitive and noncompetitive inhibition modes, overview | Homo sapiens | |
orthovanadate | competitive inhibitor | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | steady-state kinetic study, Lineweaver-Burk plots | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
[a protein]-tyrosine phosphate + H2O | Homo sapiens | - |
[a protein]-tyrosine + phosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P18031 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-nitrophenyl phosphate + H2O | - |
Homo sapiens | 4-nitrophenol + phosphate | - |
? | |
6,8-difluoro-4-methylumbelliferyl phosphate + H2O | - |
Homo sapiens | 6,8-difluoro-4-methylumbelliferol + phosphate | - |
? | |
DADE(pY)LIPQQG + H2O | sequence equivalent to residues 988-998 of the epidermal growth factor receptor | Homo sapiens | DADEYLIPQQG + phosphate | - |
? | |
[a protein]-tyrosine phosphate + H2O | - |
Homo sapiens | [a protein]-tyrosine + phosphate | - |
? | |
[epidermal growth factor receptor]-tyrosine phosphate + H2O | - |
Homo sapiens | [epidermal growth factor receptor]-tyrosine + phosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
protein tyrosine phosphatase-1B | - |
Homo sapiens |
PTP1B | - |
Homo sapiens |
tyrosine phosphatase-1B | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
22 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
5 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetic analysis of (VO2+) chelates with PTP1B, Lineweaver-Burk plots, overview | Homo sapiens | |
0.00014 | - |
bis(2-ethyl-maltolato)oxidovanadium(IV) | pH 5.0, 22°C, recombinant enzyme, versus DADE(pY)LIPQQG | Homo sapiens | |
0.00016 | - |
bis(acetylacetonato)oxidovanadium(IV) | pH 5.0, 22°C, recombinant enzyme, versus DADE(pY)LIPQQG | Homo sapiens | |
0.0003 | - |
orthovanadate | pH 5.0, 22°C, recombinant enzyme | Homo sapiens | |
0.0065 | - |
bis(acetylacetonato)oxidovanadium(IV) | pH 5.0, 22°C, recombinant enzyme, versus 4-nitrophenyl phosphate | Homo sapiens | |
0.0148 | - |
bis(2-ethyl-maltolato)oxidovanadium(IV) | pH 5.0, 22°C, recombinant enzyme, versus 4-nitrophenyl phosphate | Homo sapiens | |
0.0382 | - |
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV) | pH 5.0, 22°C, recombinant enzyme, versus 4-nitrophenyl phosphate | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
additional information | a consensus sequence H/V-C-X5-R-S/T characterizes the active sites of PTPases | Homo sapiens |