Crystallization (Comment) | Organism |
---|---|
both wild-type PTP-1B and its mutant L119V | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
G117E | mutant of PTP-1B, 45% increase in Km-value, decrease in kcat-value | Homo sapiens |
L119V | of PTP-1B, 30% decrease in kcat-value, crystallization data | Homo sapiens |
M114V | mutant of PTP-1B, activity similar to wild-type | Homo sapiens |
V113I | mutant of PTP-1B, activity similar to wild-type | Homo sapiens |
V113I/M114V | mutant of PTP-1B, 50% decrease in kcat-value | Homo sapiens |
V121L | of isoform TCPTP, high increase in sensitivity against 4-((3E)-1-(1H-benzotriazol-1-yl)-1-(4-(difluoro(phosphono)methyl)benzyl)-4-phenylbut-3-en-1-yl)benzoic acid and (difluoro(4-((4E)-2-((4-fluorophenyl)carbonyl)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-phenylpent-4-en-1-yl)phenyl)methyl)phosphonic acid | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
((4-((4E)-2-(1H-benzotriazol-1-yl)-2,5-diphenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonic acid | 50% inhibition at 109 nM for isoform PTP-1B, at 95 nM for isoform TCPTP | Homo sapiens | |
(difluoro(4-((4E)-2-((4-fluorophenyl)carbonyl)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-phenylpent-4-en-1-yl)phenyl)methyl)phosphonic acid | 50% inhibition at 163 nM for PTP-1B wild-type, at 1903 nM for PTP-1B mutant L119V, and at 1600 nM for isoform TCPTP wild-type and 138 nM for TCPTP mutant V121L | Homo sapiens | |
4-((3E)-1-(1H-benzotriazol-1-yl)-1-(4-(difluoro(phosphono)methyl)benzyl)-4-phenylbut-3-en-1-yl)benzoic acid | 50% inhibition at 39 nM for wild-type PTP-1B, at 39 nM for mutant V113I, at 45 nM for mutant M114V, at 29 nM for mutant V113I/M114V, at 32 nM for mutant G117E, at 142 nM for mutant L119V, and at 87 nM for isoform TCPTP wild-type and 24 nM for isoform TCPTP mutant V121L | Homo sapiens | |
BzN-EJJ-amide | 50% inhibition at 8nM for wild-type PTP-1B, at 14 nM for PTP-1B mutant V113I, at 7 nM for mutant M114V, at 7 nM for mutant V113I/M114V, at 11 nM for mutant G117E, at 12 nM for mutant L119V | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isoform PTP-1B and TCPTP | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
fluorescein diphosphate + H2O | - |
Homo sapiens | ? | - |
? |