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Literature summary for 3.1.3.48 extracted from

  • Peters, G.H.; Iversen, L.F.; Branner, S.; Andersen, H.S.; Mortensen, S.B.; Olsen, O.H.; Moller, K.B.; Moller, N.P.H.
    Residue 259 is a key determinant of substrate specificity of protein-tyrosine phosphatases 1B and alpha (2000), J. Biol. Chem., 275, 18201-18209.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
C258M isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition Homo sapiens
D48N isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition Homo sapiens
G259Q isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition Homo sapiens
M258C isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition Homo sapiens
N48D isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition Homo sapiens
Q259G isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition Homo sapiens
R47V isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition Homo sapiens
V47R isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0228
-
acetyl-DADEpY-NH2 pH 5.5, 30°C, PTP1B Homo sapiens
0.0246
-
acetyl-DADEpY-NH2 pH 5.5, 30°C, PTP1B, mutants R47V, D48N Homo sapiens
0.0424
-
acetyl-DADEpY-NH2 pH 5.5, 30°C, PTP1B, mutants M258C, G259Q Homo sapiens
0.219
-
acetyl-DADEpY-NH2 pH 5.5, 30°C, PTPalpha Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozymes PTP1B, PTPalpha
-

Reaction

Reaction Comment Organism Reaction ID
[a protein]-tyrosine phosphate + H2O = [a protein]-tyrosine + phosphate mechanism Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-DADEpY-NH2 + H2O
-
Homo sapiens acetyl-DADEY-NH2 + phosphate
-
?
additional information kinetic constants for several peptide substrates Homo sapiens ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2
-
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid pH 5.5, 25°C, isozyme PTP1B Homo sapiens
19
-
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid pH 5.5, 25°C, isozyme PTPalpha, mutant Q259G Homo sapiens
33
-
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid pH 5.5, 25°C, isozyme PTP1B, mutant G259Q Homo sapiens
81
-
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid pH 5.5, 25°C, isozyme PTPalpha Homo sapiens