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Literature summary for 3.1.3.48 extracted from

  • 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 (2008), Bioorg. Med. Chem., 16, 8090-8097.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.3.48

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli DH5alpha cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
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 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
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 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0027
-
 DADEpYLIPQQG wild type PTPH1, in the presence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens
0.0031
-
 DADEpYLIPQQG wild type PTPH1, in the absence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens
0.0035
-
 DADEpYLIPQQG CCPGCC-insertion mutant PTPH1-816, in the absence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens
0.0077
-
 DADEpYLIPQQG CCPGCC-insertion mutant PTPH1-816, in the presence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens
0.077
-
 DADEpYLIPQQG wild type PTPalpha, in the presence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens
0.082
-
 DADEpYLIPQQG wild type PTPalpha, in the absence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens
0.084
-
 DADEpYLIPQQG CCPGCC-insertion mutant PTPalpha-406, in the absence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens
0.1
-
 DADEpYLIPQQG CCPGCC-insertion mutant PTPalpha-406, in the presence of fluorescein arsenical hairpin binder, in 50 mM 3,3-dimethylglutarate at pH 7.0, 1 mM EDTA, and 50 mM NaCl, at 22°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P18031
-
-

Purification (Commentary)

Purification (Comment) Organism
using nickel chelated discs Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl phosphate + H2O
-
 Homo sapiens 4-nitrophenol + phosphate
-
 ?
DADEpYLIPQQG + H2O
-
 Homo sapiens DADEYLIPQQG + phosphate
-
 ?

Synonyms

Synonyms Comment Organism
Fap1
-
 Homo sapiens
HEPTP
-
 Homo sapiens
protein tyrosine phosphatase
-
 Homo sapiens
PTP
-
 Homo sapiens
PTP-PEST
-
 Homo sapiens
PTP1B
-
 Homo sapiens
PTPalpha
-
 Homo sapiens
PTPH1
-
 Homo sapiens
TCPTP
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000017
-
 fluorescein arsenical hairpin binder CCPGCC-insertion mutant TCPTP-187 Homo sapiens
0.000038
-
 fluorescein arsenical hairpin binder CCPGCC-insertion mutant PTPH1-816 Homo sapiens
0.000039
-
 fluorescein arsenical hairpin binder CCPGCC-insertion mutant PTPHalpha-406 Homo sapiens
0.000046
-
 fluorescein arsenical hairpin binder CCPGCC-insertion mutant PTP1B-186 Homo sapiens
0.000053
-
 fluorescein arsenical hairpin binder CCPGCC-insertion mutant PTP-PEST-204 Homo sapiens
0.000089
-
 fluorescein arsenical hairpin binder CCPGCC-insertion mutant HePTPH-211 Homo sapiens
0.00037
-
 fluorescein arsenical hairpin binder CCPGCC-insertion mutant FAP-1-2364 Homo sapiens