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Information on EC 3.1.3.48 - protein-tyrosine-phosphatase

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EC Tree
     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.3 Phosphoric-monoester hydrolases
                3.1.3.48 protein-tyrosine-phosphatase
IUBMB Comments
Dephosphorylates O-phosphotyrosine groups in phosphoproteins, such as the products of EC 2.7.10.2, non-specific protein-tyrosine kinase.
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This record set is specific for:
UNIPROT: P18031
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Word Map
The enzyme appears in viruses and cellular organisms
Synonyms
ptp1b, protein tyrosine phosphatase, shp-1, shp-2, tyrosine phosphatase, protein phosphatase 2a, acid phosphatase activity, mkp-1, cdc25a, ptpn22, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
low molecular weight protein tyrosine phosphatase
-
Protein phosphatase 1B
-
protein tyrosine phosphatase
-
protein tyrosine phosphatase 1B
-
protein tyrosine phosphatase, non-receptor type 1
-
protein tyrosine phosphatase-1B
-
protein-tyrosine phosphatase
-
tyrosine phosphatase-1B
-
70Z-SHP
-
-
-
-
Brain-derived phosphatase
-
-
-
-
BVP
-
-
-
-
CD148 antigen
-
-
-
-
CD45
-
-
-
-
CD45 antigen
-
-
-
-
Cdc25-like protein
-
-
-
-
CDK2-associated dual specificity phosphatase
-
-
-
-
Ch-1PTPase
-
-
-
-
CPTP1
-
-
-
-
DLAR
-
-
-
-
Dual specificity phosphatase Cdc25A
-
-
-
-
Dual specificity phosphatase Cdc25B
-
-
-
-
Dual specificity phosphatase Cdc25C
-
-
-
-
Dual specificity protein phosphatase hVH1
-
-
-
-
Dual specificity protein phosphatase hVH2
-
-
-
-
Dual specificity protein phosphatase hVH3
-
-
-
-
Dual specificity protein phosphatase PYST1
-
-
-
-
Dual specificity protein phosphatase PYST2
-
-
-
-
Dual specificity protein phosphatase VHR
-
-
-
-
Dual-specificity tyrosine phosphatase TS-DSP6
-
-
-
-
Dual-specificity tyrosine phosphatase YVH1
-
-
-
-
ES cell phosphatase
-
-
-
-
HCP
-
-
-
-
Hematopoietic cell protein-tyrosine phosphatase
-
-
-
-
Hematopoietic cell protein-tyrosine phosphatase 70Z-PEP
-
-
-
-
Hematopoietic protein-tyrosine phosphatase
-
-
-
-
HEPTP
-
-
-
-
HPTP beta-like tyrosine phosphatase
-
-
-
-
HPTP eta
-
-
-
-
hPTPE1
-
-
-
-
ICAAR
-
-
-
-
Islet cell autoantigen related protein
-
-
-
-
kinase associated phosphatase
-
-
-
-
L-CA
-
-
-
-
Late protein H1
-
-
-
-
LCA
-
-
-
-
LCA-related phosphatase
-
-
-
-
Leukocyte antigen related
-
-
-
-
Low molecular weight cytosolic acid phosphatase
-
-
-
-
LRP
-
-
-
-
Lymphoid phosphatase
-
-
-
-
LyP
-
-
-
-
M1851
-
-
-
-
MAP-kinase phosphatase CPG21
-
-
-
-
MEG
-
-
-
-
Mitosis initiation protein
-
-
-
-
Mitosis initiation protein MIH1
-
-
-
-
Mitotic inducer homolog
-
-
-
-
MKP-1 like protein tyrosine phosphatase
-
-
-
-
MPTP
-
-
-
-
MPTP-PEST
-
-
-
-
NC-PTPCOM1
-
-
-
-
Neural-specific protein-tyrosine phosphatase
-
-
-
-
ORF5
-
-
-
-
OST-PTP
-
-
-
-
P19-PTP
-
-
-
-
P80
-
-
-
-
PC12-PTP1
-
-
-
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Phogrin
-
-
-
-
Phosphacan
-
-
-
-
phosphatase, phosphoprotein (phosphotyrosine)
-
-
-
-
phosphatase, phosphotyrosine
-
-
-
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phosphoprotein phosphatase (phosphotyrosine)
-
-
-
-
phosphotyrosine histone phosphatase
-
-
-
-
phosphotyrosine phosphatase
-
-
-
-
Phosphotyrosine phosphatase 13
-
-
-
-
phosphotyrosine protein phosphatase
-
-
-
-
phosphotyrosylprotein phosphatase
-
-
-
-
protein phosphotyrosine phosphatase
-
-
-
-
Protein tyrosine phosphatase-NP
-
-
-
-
Protein-protein-tyrosine phosphatase HA2
-
-
-
-
Protein-tyrosine phosphatase 1B
-
-
-
-
Protein-tyrosine phosphatase 1C
-
-
-
-
Protein-tyrosine phosphatase 1E
-
-
-
-
Protein-tyrosine phosphatase 2C
-
-
-
-
Protein-tyrosine phosphatase 2E
-
-
-
-
Protein-tyrosine phosphatase 3CH134
-
-
-
-
Protein-tyrosine phosphatase CL100
-
-
-
-
Protein-tyrosine phosphatase D1
-
-
-
-
Protein-tyrosine phosphatase ERP
-
-
-
-
Protein-tyrosine phosphatase G1
-
-
-
-
Protein-tyrosine phosphatase H1
-
-
-
-
Protein-tyrosine phosphatase LC-PTP
-
-
-
-
Protein-tyrosine phosphatase MEG1
-
-
-
-
Protein-tyrosine phosphatase MEG2
-
-
-
-
Protein-tyrosine phosphatase P19
-
-
-
-
Protein-tyrosine phosphatase PCPTP1
-
-
-
-
Protein-tyrosine phosphatase pez
-
-
-
-
Protein-tyrosine phosphatase PTP-RL10
-
-
-
-
Protein-tyrosine phosphatase PTP36
-
-
-
-
Protein-tyrosine phosphatase PTPL1
-
-
-
-
Protein-tyrosine phosphatase striatum-enriched
-
-
-
-
Protein-tyrosine phosphatase SYP
-
-
-
-
Protein-tyrosine-phosphatase SL
-
-
-
-
Protein-tyrosine-phosphate phosphohydrolase
-
-
-
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PTP IA-2beta
-
-
-
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PTP-1B
-
-
-
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PTP-1C
-
-
-
-
PTP-1D
-
-
-
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PTP-2C
-
-
-
-
PTP-BAS
-
-
-
-
PTP-E1
-
-
-
-
PTP-H1
-
-
-
-
PTP-HA2
-
-
-
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PTP-NP
-
-
-
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PTP-SH2beta
-
-
-
-
PTP1C
-
-
-
-
PTP1D
-
-
-
-
PTP2C
-
-
-
-
PTPase YVH1
-
-
-
-
PTPase-MEG1
-
-
-
-
PTPase-MEG2
-
-
-
-
PTPG1
-
-
-
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PTPN6
-
-
-
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PTPNE6
-
-
-
-
PY protein phosphatase
-
-
-
-
R-PTP-alpha
-
-
-
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R-PTP-beta
-
-
-
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R-PTP-delta
-
-
-
-
R-PTP-epsilon
-
-
-
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R-PTP-eta
-
-
-
-
R-PTP-gamma
-
-
-
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R-PTP-kappa
-
-
-
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R-PTP-mu
-
-
-
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R-PTP-zeta
-
-
-
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Receptor-linked protein-tyrosine phosphatase 10D
-
-
-
-
Receptor-linked protein-tyrosine phosphatase 99A
-
-
-
-
RNA/RNP complex-intereracting phosphatase
-
-
-
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ROL B protein
-
-
-
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RPTPalpha
-
-
-
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SH-PTP1
-
-
-
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SH-PTP2
-
-
-
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SH-PTP3
-
-
-
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SHP
-
-
-
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Small tyrosine phosphatase
-
-
-
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Small, acidic phosphotyrosine protein phosphatase
-
-
-
-
STEP
-
-
-
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String protein
-
-
-
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Syp
-
-
-
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T-cell protein-tyrosine phosphatase
-
-
-
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T-DSP11
-
-
-
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T200
-
-
-
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TCPTP
-
-
-
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Testis-and skeletal-muscle-specific DSP
-
-
-
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tyrosine O-phosphate phosphatase
-
-
-
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Tyrosine phosphatase CBPTP
-
-
-
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tyrosylprotein phosphatase
-
-
-
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[phosphotyrosine]protein phosphatase
-
-
-
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
[a protein]-tyrosine phosphate + H2O = [a protein]-tyrosine + phosphate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of phosphoric ester
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
protein-tyrosine-phosphate phosphohydrolase
Dephosphorylates O-phosphotyrosine groups in phosphoproteins, such as the products of EC 2.7.10.2, non-specific protein-tyrosine kinase.
CAS REGISTRY NUMBER
COMMENTARY hide
79747-53-8
-
97162-86-2
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
3,6-fluorescein diphosphate + H2O
? + phosphate
show the reaction diagram
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
show the reaction diagram
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferol + phosphate
show the reaction diagram
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
show the reaction diagram
-
-
-
?
acetyl-DADEpYL-NH2 + H2O
acetyl-DADEYL-NH2 + phosphate
show the reaction diagram
-
-
?
bis-(p-phosphophenyl) methane + H2O
?
show the reaction diagram
synthetic high-affinity low-molecular weight nonpeptide substrate
-
-
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
show the reaction diagram
DADEpYLIPQQG + H2O
DADEYLIPQQG + phosphate
show the reaction diagram
-
-
-
?
difluoromethylumbelliferyl phosphate + H2O
difluoromethylumbelliferone + phosphate
show the reaction diagram
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
show the reaction diagram
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
show the reaction diagram
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
show the reaction diagram
-
-
-
?
[Eps15 peptide846-854]-tyrosine phosphate + H2O
[Eps15 peptide846-854]-tyrosine + phosphate
show the reaction diagram
active with enzyme mutant F182H, wild-type shows poor activity
-
-
?
[insulin receptor kinase]-tyrosine phosphate + H2O
[insulin receptor kinase]-tyrosine + phosphate
show the reaction diagram
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
show the reaction diagram
a physiological phosphopeptide substrate of enzyme PTP1B
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
show the reaction diagram
[insulin receptor kinase]-tyrosine phosphate + H2O
[insulin receptor kinase]-tyrosine + phosphate
show the reaction diagram
-
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((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
((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
((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
((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
((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
((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
(1R,5S,6S,6aR,7S,10S,10aS,11S)-10-(acetyloxy)-7-hydroxy-7,10a-dimethyl-4-methylidene-6-[(2-methylpropanoyl)oxy]-3-oxodecahydro-1H-1,5-methano-2-benzoxocin-11-yl 2-methylprop-2-enoate
no inhibition at 0.021 mM
(3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
-
(3aR,4R,4aR,5R,8R,8aR,9S,9aR)-8-(acetyloxy)-5-hydroxy-5,8a-dimethyl-3-methylidene-4-[(2-methylpropanoyl)oxy]-2-oxododecahydronaphtho[2,3-b]furan-9-yl 3-methylbutanoate
no inhibition at 0.020 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylprop-2-enoate
no inhibition at 0.025 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylpropanoate
no inhibition at 0.024 mM
(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
(5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid
-
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5Z)-3-benzyl-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(4-methylpent-3-en-1-yl)oxy]benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
1-(1,3-benzodioxol-5-yl)-2-([1-(4-hydroxyphenyl)-1H-1,2,3,4-tetraazol-5-yl]sulfanyl)-1-ethanone
88% inhibition at 0.2 mM
15-hydroxykaur-9(11),16-dien-19-oic acid
-
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
i.e. OATP
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-(oxalyl-amino)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxylic acid
-
2-(oxalyl-amino)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid
-
2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
i.e. TCS401, binds to the active site
2-[4,5-bis(1,3,2-dithiarsolan-2-yl)-6-hydroxy-3-oxo-3H-xanthen-9-yl]benzoic acid
i.e. FlAsH
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
mixed-type inhibition, 99% inhibition at 0.2 mM
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.008 mM, noncompetitive noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.022 mM, noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.35 mM
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
-
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide
i.e. BBR
3-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[oxalyl-amino]naphthalene-2-carboxylic acid
-
3alpha-angeloyloxypterokaurene L3
18% inhibition at 0.024 mM
3alpha-cinnamoyloxypterokaurene L3
-
3alpha-tigloyloxypterokaurene L3
no inhibition at 0.024 mM
4,6-bis(1,3,2-dithiarsolan-2-yl)-7-hydroxy-3H-phenoxazin-3-one
i.e. ReAsH
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(5-[5-(3,5-dichlorophenoxy)-2-furyl]-1,2,4-oxadiazol-3-yl)phenyl-N,N-dimethylsulfamate
85% inhibition at 0.2 mM
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5E)-5-[3-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-5-[4-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.073 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6,8-diphenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.0033 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0062 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.014 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-[(3-[(E)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-[3-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-[4-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E)-3-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]prop-1-en-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy3, 70% inhibition at 250 nM AsCy3, AsCy3 is capable of specifically and potently inhibiting mutant enzyme asPTP1B in the presence of a complex proteome, while AsCy3 does not inhibit wild-type PTP1B activity in a cell lysate
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E,5E)-5-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]penta-1,3-dien-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy5
5-chloro-2-[methyl(methylidene)-lambda4-sulfanyl]-6-[(naphthalen-2-yl)oxy]-1H-benzimidazole
65% inhibition at 0.2 mM
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
mixed-type inhibition, complete inhibition at 0.2 mM
6,8-dibenzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.013 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-((2-benzyl-1-benzothien-3-yl)methyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0032 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-((E)-1,2-diphenylvinyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0097 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-2-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.006 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0077 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.06 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0025 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.57 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.001 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.52 mM
6-(9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0071 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.036 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0043 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.002 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-bromo-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.020 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0076 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
the inhibitor is significantly selective for enzyme protein tyrosine phosphatase 1B (PTP1B) versus other phosphatases, i.e. T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase (PTP-MEG2), and src homology phosphatase 2
7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-bromoethoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-bromobutoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile
50% inhibition at 230 nM for wild-type, at 886 nM for mutant S295F
8-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.018 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0078 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(2-bromo-1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0082 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.010 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
abietic acid
a nonpolar inhibitor and weak mixed-type inhibitor of PTP1B, inhibits the enzyme by binding to its active site in a nonsubstrate-like manner that stabilizes the catalytically essential WPD loop in an inactive conformation, modelling of enzyme binding. Upon binding to the active site, abietic acid forms a hydrogen bond with R221 that weakens a bond between R221 and E115 and prevents the formation of a hydrogen bond between W179 and R221 that forms when the WPD loop closes
Berberine
binding structure, molecular modeling, overview
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)
bis(2-methyl-maltolato)oxidovanadium(IV)
-
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV)
-
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
BzN-EJJ-amide
50% inhibition at 3.7 nM for wild-type, at 18 nM for mutant S295F
continentalic acid
modelling of enzyme binding
dehydroabietic acid
modelling of enzyme binding
dihydroabietic acid
modelling of enzyme binding
ent-17-hydroxykaur-15-en-19-oic acid
40% inhibition at 0.033 mM
ent-3beta-angeloyloxykaur-16-en-19-oic acid
-
ent-3beta-tigloyloxykaur-16-en-19-oic acid
-
ent-kaur-9(11),16-dien-19-oic acid
29% inhibition at 0.033 mM
fluorescein arsenical hairpin binder
fluorescein arsenical hairpin binder does not inhibit any wild type PTP, but insertion of a fluorescein arsenical hairpin binder-binding peptide (CCPGCC) at a conserved position in the PTP catalytic-domain's WPD loop confers fluorescein arsenical hairpin binder sensitivity upon divergent PTPs
-
isopimaric acid
modelling of enzyme binding
licochalcone E
-
molybdate
competitive inhibition
MSI-1436
small molecule inhibitor MSI-1436 binds to the disordered C-terminal domain of PTP1B, C-terminal to the catalytic domain, MSI-1436 functions using an allosteric mechanism to direct the enzymatic activity of PTP1B
N-(3-chloro-4-fluorophenyl)-2-[(6,7-dimethoxy-4-oxo-3-phenyl-3,4-dihydro-2-quinazolinyl)sulfanyl]acetamide
80% inhibition at 0.2 mM
N-(3-[(3,5-difluorobenzyl)oxy]pyridin-2-yl)-4-pentylbenzenesulfonamide
74% inhibition at 0.2 mM
N-1-(2-[(2-oxo-4-propyl-2H-chromen-7-yl)oxy]propanoyl)-3-(trifluoromethyl)benzene-1-sulfonohydrazide
84% inhibition at 0.2 mM
N-[6-chloro-5-(2,3-dichlorophenoxy)-1-methyl-1H-benzimidazol-2-yl]acetamide
70% inhibition at 0.2 mM
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
mixed-type inhibition, 92% inhibition at 0.2 mM
oleanolic acid
-
orthovanadate
papaverine
binding structure, molecular modeling, overview
pterokaurene L3
no inhibition at 0.031 mM
rilobolide-6-O-methacrylate
no inhibition at 0.026 mM
tetrachyrin
-
trilobolide-6-O-isobutyrate
no inhibition at 0.026 mM
tungstate
competitive inhibition
ursolic acid
-
vanadate
the equatorial vanadate oxygen atoms bind to the P-loop and assumes a trigonal bipyramidal geometry in both transition state analogue structures, with very similar apical O-O distances, binding structure, overview
wedelolide D
32% inhibition at 0.020 mM
wedelolide H
no inhibition at 0.023 mM
wedelolide I
no inhibition at 0.021 mM
wedelolide J
no inhibition at 0.021 mM
Zn2+
low nanomolar Zn2+ concentrations inhibit isoform PTB1Bll
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,2-epoxy-3-(p-nitrophenoxy)propane
C215D mutant, not wild type
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
15 - 19
3,6-fluorescein diphosphate
0.38 - 1.1
4-nitrophenyl phosphate
0.0039
6,8-difluoro-4-methylumbelliferyl phosphate
at pH 7.4 and 25°C
1.1 - 97.5
acetyl-DADEpYL-NH2
0.0027 - 0.1
DADEpYLIPQQG
5.2 - 11.1
difluoromethylumbelliferyl phosphate
1.1 - 5.8
p-nitrophenyl phosphate
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
24.4
4-nitrophenyl phosphate
pH 5.5, 25°C
8.66
6,8-difluoro-4-methylumbelliferyl phosphate
at pH 7.4 and 25°C
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.024
4-nitrophenyl phosphate
pH 5.5, 25°C
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.023 - 0.1
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.0003 - 0.113
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.019 - 0.109
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00091 - 0.115
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00061 - 0.147
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00019 - 0.0038
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00017 - 0.088
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.0042
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
pH 7.0, 37°C
0.0052
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
pH 7.0, 37°C
0.00014 - 0.0148
bis(2-ethyl-maltolato)oxidovanadium(IV)
0.0382
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV)
pH 5.0, 22°C, recombinant enzyme, versus 4-nitrophenyl phosphate
0.00016 - 0.0065
bis(acetylacetonato)oxidovanadium(IV)
0.000017 - 0.00037
fluorescein arsenical hairpin binder
-
0.0413
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
pH 7.0, 37°C
0.0003
orthovanadate
pH 5.0, 22°C, recombinant enzyme
0.0000056
Zn2+
at pH 7.4 and 25°C
additional information
additional information
inhibition kinetic analysis of (VO2+) chelates with PTP1B, Lineweaver-Burk plots, overview
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0083
(3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
Homo sapiens
pH 6.0, 37°C
0.028
(5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid
Homo sapiens
pH 6.0, 37°C
0.0066
(5Z)-3-benzyl-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-3-benzyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0072
(5Z)-3-benzyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0206
(5Z)-3-butyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0096
(5Z)-3-butyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0298
(5Z)-5-(4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0142
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0082
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0121
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0223
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0049
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0123
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0113
(5Z)-5-(5-bromo-4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0122
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0227
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0076
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0103
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0081
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0293
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.012
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0064
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0081
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.017
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0079
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0046
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0097
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0053
(5Z)-5-[5-bromo-2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.01
(5Z)-5-[5-bromo-2-methoxy-4-[(4-methylpent-3-en-1-yl)oxy]benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.013
15-hydroxykaur-9(11),16-dien-19-oic acid
Homo sapiens
pH 6.0, 37°C
0.0084
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
Homo sapiens
pH 7.0, 37°C
0.008
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0077
3alpha-cinnamoyloxypterokaurene L3
Homo sapiens
pH 6.0, 37°C
0.01
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0042
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0051
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0019
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0071
4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0057
4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0106
4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.005
4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0109
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0025
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0104
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0022
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0051
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0056
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.003
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0014
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.018
4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0028
4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0145
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0015
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0019
4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0035
4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0019
4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0011
4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0046
4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0015
4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0038
4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0011
4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0095
4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0026
4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0011
4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0016
4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0075
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
Homo sapiens
pH 7.0, 37°C
0.003
7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0016
7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.004
7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.005
7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0079
7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.007
7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0039
7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0036
7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0069
7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0151
7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.012
ent-3beta-angeloyloxykaur-16-en-19-oic acid
Homo sapiens
pH 6.0, 37°C
0.012
ent-3beta-tigloyloxykaur-16-en-19-oic acid
Homo sapiens
pH 6.0, 37°C
0.0313
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
Homo sapiens
pH 7.0, 37°C
0.0011
rilobolide-6-O-methacrylate
Homo sapiens
pH 6.0, 37°C
0.022
tetrachyrin
Homo sapiens
pH 6.0, 37°C
0.004
ursolic acid
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4.5
mutant C215D
5.5
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
assay at
25
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
PTN1_HUMAN
435
1
49967
Swiss-Prot
other Location (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
PTPB1 possesses a P-loop, a WPD-loop, a Q-loop, a Lys-loop, and a pTyr-recognition loop, that show conformational changes during formation of the transition state
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
active site mutant C215S in complex with substrates bis-(para-phosphophenyl) methane and 4-nitrophenyl phosphate
in complex with inhibitors 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide, 3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide and 3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide
molecular dynamics simulations of the crystal structure of the enzyme catalytic domain and of mutant R47V/D48N/M258C/G259Q, both in complex with substrate 4-nitrophenyl phosphate and as cysteine-phosphor complex
PTP1B and PTP1B mutant F182H in complex with inhibitors
two transition-state analogues, by sitting drop vapor diffusion method, 4°C, mixing of 0.002 ml of protein solution, containing native PTPB1, peptide DADEYL, and Na3VO4 in 10 mM Tris, pH 7.5, 25 mM NaCl, 0.2 mM EDTA, and 3 mM DTT, with 0.0005 ml of sucrose 30% v/v solution, and 0.003 ml of precipitant solution, containing 0.1 M HEPES, pH 7.5, 0.2 M magnesium acetate and 15-17% PEG 8000, 3 days, X-ray diffraction structure determination and analysis at 2.25-2.3 A resolution
wild type and C215D mutant, both are structurally identical
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A122F
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
A122S
site-directed mutagenesis, affects inhibition by abietic acid
A189S
site-directed mutagenesis, affects inhibition by 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
C215D
active-site mutant, similar Km-values as wild type, but reduced kcat-values and activation by 1,2-epoxy-3-(p-nitrophenoxy)propane, use as substrate-trapping mutant
C215S
crystallization data, in complex with substrates bis-(para-phosphophenyl) methane and 4-nitrophenyl phosphate
C92A
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
F135Y
site-directed mutagenesis, affects inhibition by abietic acid, 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide, and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
F182H
isoform PTP1B, exchange of residue 182 with that of isoform PTPH1, modulation of functionality of catalytic center
F182Y
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
F196Y
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
F280Y
site-directed mutagenesis, does not affect abietane-type diterpenoids as inhibitors
G259S
site-directed mutagenesis, affects inhibition by 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
H175A
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
H182F
isoform PTP1B, exchange of residue 182 with that of isoform PTPB1, modulation of functionality of catalytic center
P87C/A122C
mutant asPTP1B, design of non-natural allosteric-inhibition sites in PTPs, in which a tricysteine moiety is engineered within the PTP catalytic domain at a conserved location outside of the active site. Introduction of the tricysteine motif, which does not exist in any wild-type PTP, serves to sensitize target PTPs to inhibition by a biarsenical compound, providing a generalizable strategy for the generation of allosterically sensitized (as) PTPs. The potency, selectivity, and kinetics of asPTP inhibition can be significantly improved by exploring the inhibitory action of a range of biarsenical compounds that differ in interarsenical distance, steric bulk, and electronic structure
R112A
site-directed mutagenesis, affects inhibition by abietic acid, 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide, and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
R47V/D48N/M258C/G259Q
molecular dynamics simulations of the crystal structure, in comparison to wild-type, movement of Q262 is restricted
S295F
affects minimally catalytic activity, significantly reduces the potency of inhibitors derived from 7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile
V113T
site-directed mutagenesis, does not affect abietane-type diterpenoids as inhibitors
W179F
site-directed mutagenesis, the mutation in PTP1B causes only a minor reduction in kcat of about 2fold at pH 5.5, and the pH-rate profile remains fully bell-shaped. The kinetic isotopic effects are similar to those of the wild-type PTP1B showing that general acid catalysis remains effective. The affinity of the competitive inhibitors tungstate and molybdate for the active site is not affected by the W179F mutation. Crystal structures of the W179F mutant of PTP1B show the availability of both the normal loop open and closed positions, consistent with the kinetic results
Y152A/Y153A
site-directed mutagenesis, the mutation attenuates allosteric communication between the C-terminus and the WPD loop, affects inhibition by abietic acid, 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide, and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
Y46A
site-directed mutagenesis, substitution of Y46 with alalnine in PTP1B results in a 380fold increase in Km using pNPP as a substrate
additional information
the mutants TCPTP-187 , PTP1B-186, HePTP-211, FAP-1-2364 , PTP-PEST-204 have a CCPGCC-insertion that leads to sensitisation toward fluorescein arsenical hairpin binder protein, the CCPGCC-insertion mutants PTPH1-816 and PTPalpha-406 are particularly attractive as inhibitor-sensitized enzymes in that they demonstrate kinetic parameters that are essentially indistinguishable (or marginally improved, in the case of PTPalpha-406) from the corresponding wild type enzymes in the absence of an allele-specific inhibitor
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromatography
using nickel chelated discs
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli DH5alpha cells
gene PTP1B, recombinant expression of C-terminally His-tagged wild-type and mutant enzymes (PTP1B residues 1-321) in Escherichia coli strain BL21(DE3)
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
the enzyme is a target for inhibitor design
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Pedersen, A.K.; Guo, X.L.; Moller, K.B.; Peters, G.H.; Andersen, H.S.; Kastrup, J.S.; Mortensen, S.B.; Iversen, L.F.; Zhang, Z.Y.; Moller, N.P.H.
Residue 182 influences the second step of protein-tyrosine phosphatase-mediated catalysis
Biochem. J.
378
421-433
2004
Homo sapiens (P18031)
Manually annotated by BRENDA team
Romsicki, Y.; Scapin, G.; Beaulieu-Audy, V.; Patel, S.; Becker, J.W.; Kennedy, B.P.; Asante-Appiah, E.
Functional characterization and crystal structure of the C215D mutant of protein-tyrosine phosphatase-1B
J. Biol. Chem.
278
29009-29015
2003
Homo sapiens (P18031)
Manually annotated by BRENDA team
Peters, G.H.; Iversen, L.F.; Andersen, H.S.; Moller, N.P.; Olsen, O.H.
Residue 259 in protein-tyrosine phosphatase PTP1B and PTPalpha determines the flexibility of glutamine 262
Biochemistry
43
8418-8428
2004
Homo sapiens (P18031)
Manually annotated by BRENDA team
Shim, Y.S.; Kim, K.C.; Lee, K.A.; Shrestha, S.; Lee, K.H.; Kim, C.K.; Cho, H.
Formylchromone derivatives as irreversible and selective inhibitors of human protein tyrosine phosphatase 1B. Kinetic and modeling studies
Bioorg. Med. Chem.
13
1325-1332
2005
Homo sapiens (P18031), Homo sapiens
Manually annotated by BRENDA team
Puius, Y.A.; Zhao, Y.; Sullivan, M.; Lawrence, D.S.; Almo, S.C.; Zhang, Z.Y.
Identification of a second aryl phosphate-binding site in protein-tyrosine phosphatase 1B: a paradigm for inhibitor design
Proc. Natl. Acad. Sci. USA
94
13420-13425
1997
Homo sapiens (P18031), Homo sapiens
Manually annotated by BRENDA team
Lund, I.K.; Andersen, H.S.; Iversen, L.F.; Olsen, O.H.; Moller, K.B.; Pedersen, A.K.; Ge, Y.; Holsworth, D.D.; Newman, M.J.; Axe, F.U.; Moller, N.P.
Structure-based design of selective and potent inhibitors of protein-tyrosine phosphatase beta
J. Biol. Chem.
279
24226-24235
2004
Homo sapiens (P18031), Homo sapiens
Manually annotated by BRENDA team
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
J. Biol. Chem.
281
5258-5266
2006
Homo sapiens (P18031)
Manually annotated by BRENDA team
Wiesmann, C.; Barr, K.J.; Kung, J.; Zhu, J.; Erlanson, D.A.; Shen, W.; Fahr, B.J.; Zhong, M.; Taylor, L.; Randal, M.; McDowell, R.S.; Hansen, S.K.
Allosteric inhibition of protein tyrosine phosphatase 1B
Nat. Struct. Mol. Biol.
11
730-737
2004
Homo sapiens (P18031), Homo sapiens
Manually annotated by BRENDA team
Zhang, X.Y.; Chen, V.L.; Rosen, M.S.; Blair, E.R.; Lone, A.M.; Bishop, A.C.
Allele-specific inhibition of divergent protein tyrosine phosphatases with a single small molecule
Bioorg. Med. Chem.
16
8090-8097
2008
Homo sapiens (P18031)
Manually annotated by BRENDA team
Hendriks, W.J.; Elson, A.; Harroch, S.; Stoker, A.W.
Protein tyrosine phosphatases: functional inferences from mouse models and human diseases
FEBS J.
275
816-830
2008
Homo sapiens, Homo sapiens (O14522), Homo sapiens (P10586), Homo sapiens (P17706), Homo sapiens (P18031), Homo sapiens (P18433), Homo sapiens (P23467), Homo sapiens (P23468), Homo sapiens (P23469), Homo sapiens (P23470), Homo sapiens (P23471), Homo sapiens (P26045), Homo sapiens (P28827), Homo sapiens (P29074), Homo sapiens (P29350), Homo sapiens (P35236), Homo sapiens (P43378), Homo sapiens (P54829), Homo sapiens (Q05209), Homo sapiens (Q06124), Homo sapiens (Q0VAE8), Homo sapiens (Q12913), Homo sapiens (Q12923), Homo sapiens (Q13332), Homo sapiens (Q15256), Homo sapiens (Q15262), Homo sapiens (Q15678), Homo sapiens (Q16825), Homo sapiens (Q16827), Homo sapiens (Q16849), Homo sapiens (Q4JDK3), Homo sapiens (Q92729), Homo sapiens (Q92932), Homo sapiens (Q99952), Homo sapiens (Q9H3S7), Homo sapiens (Q9HD43), Homo sapiens (Q9UMZ3), Homo sapiens (Q9Y2R2)
Manually annotated by BRENDA team
Bustanji, Y.; Taha, M.O.; Al-Masri, I.M.; Mohammad, M.K.
Docking simulations and in vitro assay unveil potent inhibitory action of papaverine against protein tyrosine phosphatase 1B
Biol. Pharm. Bull.
32
640-645
2009
Homo sapiens (P18031), Homo sapiens
Manually annotated by BRENDA team
Maccari, R.; Ottana, R.; Ciurleo, R.; Paoli, P.; Manao, G.; Camici, G.; Laggner, C.; Langer, T.
Structure-based optimization of benzoic acids as inhibitors of protein tyrosine phosphatase 1B and low molecular weight protein tyrosine phosphatase
ChemMedChem
4
957-962
2009
Homo sapiens (P18031)
Manually annotated by BRENDA team
Brandao, T.A.; Hengge, A.C.; Johnson, S.J.
Insights into the reaction of protein tyrosine phosphatase 1B. Crystal structures for transition-state analogs of both catalytic steps
J. Biol. Chem.
285
15874-15883
2010
Homo sapiens (P18031)
Manually annotated by BRENDA team
Wang, Z.; Liu, Z.; Lee, W.; Kim, S.N.; Yoon, G.; Cheon, S.H.
Design, synthesis and docking study of 5-(substituted benzylidene)thiazolidine-2,4-dione derivatives as inhibitors of protein tyrosine phosphatase 1B
Bioorg. Med. Chem. Lett.
24
3337-3340
2014
Homo sapiens (P18031)
Manually annotated by BRENDA team
Bellomo, E.; Massarotti, A.; Hogstrand, C.; Maret, W.
Zinc ions modulate protein tyrosine phosphatase 1B activity
Metallomics
6
1229-1239
2014
Homo sapiens (P18031), Homo sapiens
Manually annotated by BRENDA team
Li, S.; Zhang, J.; Lu, S.; Huang, W.; Geng, L.; Shen, Q.; Zhang, J.
The mechanism of allosteric inhibition of protein tyrosine phosphatase 1B
PLoS ONE
9
e97668
2014
Homo sapiens (P18031)
Manually annotated by BRENDA team
Hjortness, M.; Riccardi, L.; Hongdusit, A.; Ruppe, A.; Zhao, M.; Kim, E.; Zwart, P.; Sankaran, B.; Arthanari, H.; Sousa, M.; De Vivo, M.; Fox, J.
Abietane-type diterpenoids inhibit protein tyrosine phosphatases by stabilizing an inactive enzyme conformation
Biochemistry
57
5886-5896
2018
Homo sapiens (P18031)
-
Manually annotated by BRENDA team
Hengge, A.C.
Kinetic isotope effects in the characterization of catalysis by protein tyrosine phosphatases
Biochim. Biophys. Acta
1854
1768-1775
2015
Yersinia sp., Homo sapiens (P18031), Homo sapiens (P51452), Homo sapiens (Q9BVJ7), Mus musculus (P35821), Schizosaccharomyces pombe (P41893), Schizosaccharomyces pombe ATCC 24843 (P41893)
Manually annotated by BRENDA team
Zhang, L.; Ge, Y.; Song, H.M.; Wang, Q.M.; Zhou, C.H.
Design, synthesis of novel azolyl flavonoids and their protein tyrosine Phosphatase-1B inhibitory activities
Bioorg. Chem.
80
195-203
2018
Homo sapiens (P18031)
Manually annotated by BRENDA team
Peti, W.; Page, R.
Strategies to make protein serine/threonine (PP1, calcineurin) and tyrosine phosphatases (PTP1B) druggable Achieving specificity by targeting substrate and regulatory protein interaction sites
Bioorg. Med. Chem.
23
2781-2785
2015
Homo sapiens (P18031)
Manually annotated by BRENDA team
Korntner, S.; Pomorski, A.; Krezel, A.; Bishop, A.C.
Optimized allosteric inhibition of engineered protein tyrosine phosphatases with an expanded palette of biarsenical small molecules
Bioorg. Med. Chem.
26
2610-2620
2018
Homo sapiens (P18031)
Manually annotated by BRENDA team
Abdjul, D.B.; Yamazaki, H.; Kanno, S.I.; Kirikoshi, R.; Tomizawa, A.; Takahashi, O.; Maarisit, W.; Losung, F.; Rotinsulu, H.; Wewengkang, D.S.; Sumilat, D.A.; Kapojos, M.M.; Namikoshi, M.
Absolute structures of wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes from aerial parts of Wedelia spp. collected in Indonesia and Japan
Chem. Pharm. Bull.
66
682-687
2018
Homo sapiens (P18031), Homo sapiens
Manually annotated by BRENDA team
Ottana, R.; Paoli, P.; Nass, A.; Lori, G.; Cardile, V.; Adornato, I.; Rotondo, A.; Graziano, A.C.E.; Wolber, G.; Maccari, R.
Discovery of 4-[(5-arylidene-4-oxothiazolidin-3-yl)methyl]benzoic acid derivatives active as novel potent allosteric inhibitors of protein tyrosine phosphatase 1B in silico studies and in vitro evaluation as insulinomimetic and anti-inflammatory agents
Eur. J. Med. Chem.
127
840-858
2017
Homo sapiens (P18031)
Manually annotated by BRENDA team
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
J. Biol. Inorg. Chem.
22
1267-1279
2017
Homo sapiens (P18031)
Manually annotated by BRENDA team
Sarabia-Sanchez, M.J.; Trejo-Soto, P.J.; Velazquez-Lopez, J.M.; Carvente-Garcia, C.; Castillo, R.; Hernandez-Campos, A.; Avitia-Dominguez, C.; Enriquez-Mendiola, D.; Sierra-Campos, E.; Valdez-Solana, M.; Salas-Pacheco, J.M.; Tellez-Valencia, A.
Novel mixed-type inhibitors of protein tyrosine phosphatase 1B. Kinetic and computational studies
Molecules
22
2262-2278
2017
Homo sapiens (P18031)
Manually annotated by BRENDA team
Chen, K.E.; Li, M.Y.; Chou, C.C.; Ho, M.R.; Chen, G.C.; Meng, T.C.; Wang, A.H.
Substrate specificity and plasticity of FERM-containing protein tyrosine phosphatases
Structure
23
653-664
2015
Homo sapiens (P18031), Homo sapiens (P26045), Homo sapiens (Q12923), Homo sapiens (Q15678), Homo sapiens (Q16825)
Manually annotated by BRENDA team