Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.1.3.48 extracted from

  • Hon, J.; Hwang, M.S.; Charnetzki, M.A.; Rashed, I.J.; Brady, P.B.; Quillin, S.; Makinen, M.W.
    Kinetic characterization of the inhibition of protein tyrosine phosphatase-1B by vanadyl (VO2+) chelates (2017), J. Biol. Inorg. Chem., 22, 1267-1279 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.3.48

Inhibitors

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 [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information steady-state kinetic study, Lineweaver-Burk plots Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens P18031
-
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
protein tyrosine phosphatase-1B
-
 Homo sapiens
PTP1B
-
 Homo sapiens
tyrosine phosphatase-1B
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5
-
 assay at Homo sapiens

Ki Value [mM]

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

General Information Comment Organism
additional information a consensus sequence H/V-C-X5-R-S/T characterizes the active sites of PTPases Homo sapiens