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Literature summary for 3.1.3.48 extracted from

  • Eswaran, J.; von Kries, J.P.; Marsden, B.; Longman, E.; Debreczeni, J.E.; Ugochukwu, E.; Turnbull, A.; Lee, W.H.; Knapp, S.; Barr, A.J.
    Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases (2006), Biochem. J., 395, 483-491.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting drop vapour diffusion method using 25% PEG-3350, 0.2 M LiSO4, and 100 mM Bis-Tris, pH 5.5, or 0.15 M malic acid, pH 7.0, 20% PEG-3350 and 2.0 M (NH4)H2PO4, 0.1 M Tris/HCl, pH 8.5 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(2,5-dimethyl-1H-pyrrol-1-yl)-5-hydroxybenzoic acid 36% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 7% residual activity at 0.1 mM; 9% residual activity at 0.1 mM Homo sapiens
2-chloro-4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 36% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 95% residual activity at 0.1 mM; 98% residual activity at 0.1 mM Homo sapiens
2-chloro-5-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 37% residual activity at 0.1 mM; 77% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 91% residual activity at 0.1 mM Homo sapiens
3-(2,5-dimethyl-1H-pyrrol-1-yl)-4-hydroxybenzoic acid 20% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 52% residual activity at 0.1 mM; 7% residual activity at 0.1 mM Homo sapiens
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,6-dicarboxylic acid 25% residual activity at 0.1 mM; 39% residual activity at 0.1 mM; 65% residual activity at 0.1 mM; 73% residual activity at 0.1 mM Homo sapiens
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,8-dicarboxylic acid 30% residual activity at 0.1 mM; 53% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 79% residual activity at 0.1 mM Homo sapiens
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 23% residual activity at 0.1 mM; 75% residual activity at 0.1 mM; 80% residual activity at 0.1 mM; 9% residual activity at 0.1 mM Homo sapiens
4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 63% residual activity at 0.1 mM; 6% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 9% residual activity at 0.1 mM Homo sapiens
4-(2,5-dimethyl-1H-pyrrol-1-yl)-3-hydroxybenzoic acid 21% residual activity at 0.1 mM; 67% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 9% residual activity at 0.1 mM Homo sapiens
4-(2,5-dimethyl-1H-pyrrol-1-yl)phthalic acid 18% residual activity at 0.1 mM; 54% residual activity at 0.1 mM; 78% residual activity at 0.1 mM; 80% residual activity at 0.1 mM Homo sapiens
5-acetylamino-2-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 45% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 82% residual activity at 0.1 mM; 94% residual activity at 0.1 mM Homo sapiens
6-fluoro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 35% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 75% residual activity at 0.1 mM Homo sapiens
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylate 80% residual activity at 0.1 mM Homo sapiens
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 38% residual activity at 0.1 mM; 50% residual activity at 0.1 mM; 73% residual activity at 0.1 mM Homo sapiens
8-acetyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 48% residual activity at 0.1 mM; 66% residual activity at 0.1 mM; 81% residual activity at 0.1 mM; 83% residual activity at 0.1 mM Homo sapiens
8-bromo-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 33% residual activity at 0.1 mM; 41% residual activity at 0.1 mM; 8% residual activity at 0.1 mM; 90% residual activity at 0.1 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni2+-Sepharose affinity HiTrap HP column chromatography, Superdex 200 16/60 gel filtration, DEAE-cellulose resin chromatography, and HiTrapQ column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
-
Homo sapiens 6,8-difluoro-4-methylumbelliferone + phosphate
-
?
p-nitrophenyl phosphate
-
Homo sapiens p-nitrophenol + phosphate
-
?

Subunits

Subunits Comment Organism
monomer x-ray crystallography Homo sapiens

Synonyms

Synonyms Comment Organism
protein tyrosine phosphatase
-
Homo sapiens
PTP1B
-
Homo sapiens
PTPN5
-
Homo sapiens
PTPN7
-
Homo sapiens
PTPRR
-
Homo sapiens
STEP
-
Homo sapiens
striatal-enriched PTP
-
Homo sapiens