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Literature summary for 3.1.3.48 extracted from

  • Forghieri, M.; Laggner, C.; Paoli, P.; Langer, T.; Manao, G.; Camici, G.; Bondioli, L.; Prati, F.; Costantino, L.
    Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors (2009), Bioorg. Med. Chem., 17, 2658-2672.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid no inhibition of LMW-PTP isozymes, but 20% inhibition of PTP-B1 at 0.02 mM Homo sapiens
2',4'-dihydroxy-1,1'-biphenyl
-
Homo sapiens
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
3',4'-dihydroxy-1,1'-biphenyl no inhibition of LMW-PTP isozymes, but 5% inhibition of PTP-B1 at 0.02 mM Homo sapiens
3-(biphenyl-4-ylmethyl)-6-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
-
Homo sapiens
3-benzyl-7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one 10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM Homo sapiens
4'-carboxy-3'-hydroxy-1,1'-biphenyl no inhibition of LMW-PTP isozymes, but 10% inhibition of PTP-B1 at 0.02 mM Homo sapiens
4'-[(2-butyl-1-benzofuran-3-yl)methyl]biphenyl-4-ol
-
Homo sapiens
4'-[2-(4-hydroxybutyl)-1-benzofuran-3-yl]biphenyl-4-ol
-
Homo sapiens
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 20% inhibition of PTP-B1 at 0.015 mM Homo sapiens
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
Homo sapiens
7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one 10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM Homo sapiens
7-hydroxy-2-(4-hydroxyphenyl)-3-[(3',4'-dihydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one 60% inhibition of LMW-PTP isozyme 2, 25% inhibition of LMW-PTP 1, and 50% inhibition of PTP-B1, at 0.02 mM Homo sapiens
7-hydroxy-2-(4-hydroxyphenyl)-3-[(4'-carboxy-3'-hydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one 5% inhibition of LMW-PTP isozyme 2, 10% inhibition of LMW-PTP 1, and 59% inhibition of PTP-B1, at 0.02 mM Homo sapiens
7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 20% inhibition of PTP-B1 at 0.015 mM Homo sapiens
7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 10% inhibition of PTP-B1 at 0.015 mM Homo sapiens
7-hydroxy-2-(4-hydroxyphenylpropyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM Homo sapiens
biphenyl-3,4-diol 25% inhibition of LMW-PTP isozyme 2, and 10% inhibition of LMW-PTP 1 and PTP-B1 at 0.02 mM Homo sapiens
[[4'-(2-butyl-1-benzofuran-3-yl)biphenyl-4-yl]oxy]acetic acid
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P24666 two isozymes of LMW-PTP, and PTP-1B
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl phosphate + H2O
-
Homo sapiens 4-nitrophenol + phosphate
-
?

Synonyms

Synonyms Comment Organism
LMW-PTP
-
Homo sapiens
More the enzyme belongs to the LMW-PTP family Homo sapiens
protein tyrosine phosphatase
-
Homo sapiens
PTP
-
Homo sapiens
PTP-1B
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0007
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.00074
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 2',4'-dihydroxy-1,1'-biphenyl
0.0009
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.001
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.00108
-
pH 7.0, 37°C, PTP-B2 Homo sapiens 4'-[2-(4-hydroxybutyl)-1-benzofuran-3-yl]biphenyl-4-ol
0.0011
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.00119
-
pH 7.0, 37°C, PTP-B3 Homo sapiens 4'-[(2-butyl-1-benzofuran-3-yl)methyl]biphenyl-4-ol
0.0013
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.002
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.00219
-
pH 7.0, 37°C, PTP-B4 Homo sapiens [[4'-(2-butyl-1-benzofuran-3-yl)biphenyl-4-yl]oxy]acetic acid
0.0022
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.003
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.005
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0053
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0057
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0062
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0065
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0074
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0077
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0082
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0086
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0114
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0124
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0126
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0143
-
pH 7.0, 37°C, LMW-PTP isozyme 1 Homo sapiens 2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.017
-
pH 7.0, 37°C, PTP-B1 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0172
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0173
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0175
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0184
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0268
-
pH 7.0, 37°C, LMW-PTP isozyme 2 Homo sapiens 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one

General Information

General Information Comment Organism
physiological function protein tyrosine phosphatases are crucial elements in eukaryotic signal transduction Homo sapiens