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

BRENDA support

Literature summary for 3.1.3.48 extracted from

  • Montalibet, J.; Skorey, K.; McKay, D.; Scapin, G.; Asante-Appiah, E.; Kennedy, B.P.
    Residues distant from the active site influence protein-tyrosine phosphatase 1B inhibitor binding (2006), J. Biol. Chem., 281, 5258-5266.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
S295F affects minimally catalytic activity, significantly reduces the potency of inhibitors derived from 7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
((2-bromo-4-((((2E)-3-phenylprop-2-en-1-yl)sulfanyl)methyl)phenyl)carbonyl)phosphonate 50% inhibition at 810 nM for wild-type, at 1290 nM for mutant S295F Homo sapiens
((2-bromo-4-(((4-chlorobenzyl)thio)methyl)phenyl)(difluoro)methyl)phosphonate 50% inhibition at 285 nM for wild-type, at 1644 nM for mutant S295F Homo sapiens
((2-phenyl-2-(phenylcarbonyl)propane-1,3-diyl)bis(benzene-4,1-diyl(difluoromethanediyl)))bis(phosphonate) 50% inhibition at 82 nM for wild-type, at 399 nM for mutant S295F Homo sapiens
((4-((((3'-(acetylsulfamoyl)biphenyl-4-yl)methyl)sulfanyl)methyl)-2-bromophenyl)(difluoro)methyl)phosphonate 50% inhibition at 2.2 nM for wild-type, at 11 nM for mutant S295F Homo sapiens
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonate 50% inhibition at 47 nM for wild-type, at 260 nM for mutant S295F Homo sapiens
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(fluoro)methyl)phosphonate 50% inhibition at 570 nM for wild-type, at 830 nM for mutant S295F Homo sapiens
(4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)benzyl)phosphonate 50% inhibition at 3260 nM for wild-type, at 5030 nM for mutant S295F Homo sapiens
7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile 50% inhibition at 230 nM for wild-type, at 886 nM for mutant S295F Homo sapiens
BzN-EJJ-amide 50% inhibition at 3.7 nM for wild-type, at 18 nM for mutant S295F Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.38
-
4-nitrophenyl phosphate wild-type, pH 6.3 Homo sapiens
1.1
-
4-nitrophenyl phosphate mutant S295F, pH 6.3 Homo sapiens
5.2
-
difluoromethylumbelliferyl phosphate wild-type, pH 6.3 Homo sapiens
11.1
-
difluoromethylumbelliferyl phosphate mutant S295F, pH 6.3 Homo sapiens
15
-
3,6-fluorescein diphosphate mutant S295F, pH 6.3 Homo sapiens
19
-
3,6-fluorescein diphosphate wild-type, pH 6.3 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P18031 isoform PTP1B, amino acids 1-400, catalytic domain plus 80-amino acid C-terminal tail
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3,6-fluorescein diphosphate + H2O
-
Homo sapiens ? + phosphate
-
?
4-nitrophenyl phosphate + H2O
-
Homo sapiens 4-nitrophenol + phosphate
-
?
difluoromethylumbelliferyl phosphate + H2O
-
Homo sapiens difluoromethylumbelliferone + phosphate
-
?