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Literature summary extracted from

  • Lountos, G.; Kurussi, S.; Zhao, B.; Dyas, B.; Burke, T.J.; Ulrich, R.; Waugh, D.
    High-resolution crystal structures of the D1 and D2 domains of protein tyrosine phosphatase epsilon for structure-based drug design (2018), Acta Crystallogr. Sect. D, 74, 1015-1026 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.3.48 recombinant expression of the TEV protease-cleavable, N-terminally His6-tagged maltose-binding protein-PTPepsilon D1(Ser107-Gly398) fusion protein and of wild-type and mutant TEV protease-cleavable, N-terminally His6-tagged-maltose-binding protein D2 domain of PTPepsilon D2(Gly425-Lys700) in Escherichia coli strain Rosetta 2 (DE3) Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.1.3.48 purified recombinant wild-type and mutant isolated membrane-proximal D1 and distal D2 domains of protein tyrosine phosphatase epsilon, and PTPepsilon (A455N/V457Y/E597D) D2 domain mutant, hanging drop vapour diffusion method, for PTPepsilon D1 domain mixing of 0.002 ml of 13.9 mg/ml protein solution with 0.002 ml of reservoir solution containing 0.1 M Tris-HCl, pH 8.5, 0.2 M sodium chloride, and 22% w/v PEG 3350, for wild-type PTPepsilon D2 domain mixing of 0.001 ml of 5.0 mg/ml protein solution with 0.003 ml of reservoir solution containing 0.1 M bicine/trizma base, pH 8.5, 0.03 mM diethylene glycol, 0.03 M triethylene glycol, 0.03 M tetraethylene glycol, 0.03 M pentaethylene glycol, 10% w/v PEG 4000, and 20% v/v glycerol, and for mutant A455N/V457Y/E597D PTPepsilon D2 domain mixing of 0.002 ml of 9.0 mg/ml protein solution with 0.002 ml of reservoir solution containing 0.1 M imidazole, pH 8.0, 0.2 M calcium acetate hydrate, 20% w/v PEG 1000, in all cases equilibration against 0.5 ml reservoir solution, X-ray diffraction structure determination and analysis at 1.67-2.27 A resolution Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.1.3.48 A455N/V457Y/E597D site-directed mutagenesis, the triple mutant of the PTPepsilon D2 domain is constructed to reconstitute the residues of the PTPepsilon D1 catalytic domain that are important for phosphatase activity, resulting in only a slight increase in the phosphatase activity compared with the wild-type D2 protein. The mutant is used for structure-based drug design Homo sapiens
3.1.3.48 V457Y/E597D site-directed mutagenesis Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.3.48 additional information structure-based drug design Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.3.48 0.119
-
PQDKEY-pY-KVKEPG pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a JAK2 peptide Homo sapiens
3.1.3.48 0.124
-
RKGSGD-pY-MPMSPK pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a IRS1 peptide Homo sapiens
3.1.3.48 0.127
-
PGSAAP-pY-LKTKFI pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a STAT3 peptide Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.1.3.48 plasma membrane
-
Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.3.48 [a protein]-tyrosine phosphate + H2O Homo sapiens
-
[a protein]-tyrosine + phosphate
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.1.3.48 Homo sapiens P23469
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.3.48 recombinant wild-type and mutant TEV protease-cleavable, N-terminally His6-tagged maltose-binding protein-PTPepsilon D1 and D2 fusion proteins from Escherichia coli strain Rosetta 2 (DE3) by nickel affinity chromatography, ultrafiltration, and cleavage of the tag/fusion protein, followed by gel filtration and ultrafiltration Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.3.48 breast cancer cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.3.48 additional information activity detection by malachite green phosphatase method for phosphate determination Homo sapiens ?
-
?
3.1.3.48 PGSAAP-pY-LKTKFI + H2O STAT3 peptide Homo sapiens PGSAAPYLKTKFI + phosphate
-
?
3.1.3.48 PQDKEY-pY-KVKEPG + H2O JAK2 peptide Homo sapiens PQDKEYYKVKEPG + phosphate
-
?
3.1.3.48 RKGSGD-pY-MPMSPK + H2O IRS1 peptide Homo sapiens RKGSGDYMPMSPK + phosphate
-
?
3.1.3.48 [a protein]-tyrosine phosphate + H2O
-
Homo sapiens [a protein]-tyrosine + phosphate
-
?

Subunits

EC Number Subunits Comment Organism
3.1.3.48 More the receptor PTPepsilon is located in the plasma membrane and possesses a small extracellular domain, a membrane-spanning domain and two tandem cytoplasmic domains, D1 and D2 Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
3.1.3.48 protein tyrosine phosphatase epsilon
-
Homo sapiens
3.1.3.48 PTPepsilon
-
Homo sapiens
3.1.3.48 receptor PTPepsilon
-
Homo sapiens
3.1.3.48 RPTPepsilon
-
Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.3.48 22 25 assay at Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.1.3.48 3.1
-
PQDKEY-pY-KVKEPG pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a JAK2 peptide Homo sapiens
3.1.3.48 3.2
-
RKGSGD-pY-MPMSPK pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a IRS1 peptide Homo sapiens
3.1.3.48 3.6
-
PGSAAP-pY-LKTKFI pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a STAT3 peptide Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.3.48 6.4
-
assay at Homo sapiens

General Information

EC Number General Information Comment Organism
3.1.3.48 additional information PTPepsilon D1 and D2 active site structures, overview Homo sapiens
3.1.3.48 physiological function the reversible phosphorylation of tyrosine residues in proteins, which depends on the balanced coordination between a multitude of protein tyrosine kinases (PTKs) and protein tyrosine phosphatases (PTPs), is an essential step in many cellular signaling pathways. Classical type I cysteine-based PTPs include both receptor and nonreceptor forms that catalyze the removal of the phosphate moiety from a targeted pTyr residue. The enzyme plays a positive role in the survival of human breast cancer cells Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.1.3.48 25.81
-
RKGSGD-pY-MPMSPK pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a IRS1 peptide Homo sapiens
3.1.3.48 26.05
-
PQDKEY-pY-KVKEPG pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a JAK2 peptide Homo sapiens
3.1.3.48 28.35
-
PGSAAP-pY-LKTKFI pH 6.4, 25°C, recombinant PTPepsilon D1 domain, substrate is a STAT3 peptide Homo sapiens