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Literature summary for 3.1.3.48 extracted from

  • Wiesmann, C.; Barr, K.J.; Kung, J.; Zhu, J.; Erlanson, D.A.; Shen, W.; Fahr, B.J.; Zhong, M.; Taylor, L.; Randal, M.; McDowell, R.S.; Hansen, S.K.
    Allosteric inhibition of protein tyrosine phosphatase 1B (2004), Nat. Struct. Mol. Biol., 11, 730-737.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide, 3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide and 3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide 50% inhibition of PTP1B at 0.008 mM, noncompetitive noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop Homo sapiens
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide 50% inhibition of PTP1B at 0.022 mM, noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop Homo sapiens
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide 50% inhibition of PTP1B at 0.35 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P18031 isoform PTP1B
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