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Literature summary for 3.1.3.48 extracted from

  • Park, J.; Pei, D.
    Trans-b-nitrostyrene derivatives as slow-binding inhibitors of protein tyrosine phosphatases (2004), Biochemistry, 43, 15014-15021.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
((1E)-2-nitroprop-1-en-1-yl)benzene 50% inhibition at 0.023 mM in absence of 2-mercaptoethanol, at 0.515 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens
((E)-2-nitrovinyl)benzene i.e. trans-beta-nitrostyrene, slow-binding inhibitor, acting as a pY mimetic and binding to the enzyme active site to form an initial noncovalent E*I complex, followed by nucleophilic attack on the nitrostyrene nitro group by C215 of enzyme to form a reversible, covalent adduct. 50% inhibition at 0.0025 mM in absence of 2-mercaptoethanol, at 0.4 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens
1,3-difluoro-2-[(E)-2-nitroethenyl]benzene 50% inhibition at 0.0048 mM in absence of 2-mercaptoethanol, at 0.34 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens
1-methoxy-4-((E)-2-nitrovinyl)benzene 50% inhibition at 0.0045 mM in absence of 2-mercaptoethanol, at 0.27 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens
1-methyl-4-((E)-2-nitrovinyl)benzene 50% inhibition at 0.003 mM in absence of 2-mercaptoethanol, at 0.225 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens
2,4-dimethoxy-1-((E)-2-nitrovinyl)benzene 50% inhibition at 0.028 mM in absence of 2-mercaptoethanol, at 0.390 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens
4-((E)-2-nitrovinyl)benzoic acid 50% inhibition at 0.0027 mM in absence of 2-mercaptoethanol, at 0.425 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens
N-((4-((E)-2-nitroethenyl)phenyl)carbonyl)glycyl-L-alpha-glutamyl-L-glutamic acid 50% inhibition at 0.0014 mM in absence of 2-mercaptoethanol, at 0.275 mM in presence of 1 mM 2-mercaptoethanol Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isoform PTP1B, recombinant enzyme
-