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

BRENDA support

Literature summary for 3.1.3.48 extracted from

  • Asante-Appiah, E.; Patel, S.; Desponts, C.; Taylor, J.M.; Lau, C.; Dufresne, C.; Therien, M.; Friesen, R.; Becker, J.W.; Leblanc, Y.; Kennedy, B.P.; Scapin, G.
    Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase (2006), J. Biol. Chem., 281, 8010-8015.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
both wild-type PTP-1B and its mutant L119V Homo sapiens

Protein Variants

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

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

Organism UniProt Comment Textmining
Homo sapiens
-
isoform PTP-1B and TCPTP
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
fluorescein diphosphate + H2O
-
Homo sapiens ?
-
?