Thiophosphorylated substrate analogs are potent active site-directed inhibitors of protein-tyrosine phosphatases.

@article{Hiriyanna1994ThiophosphorylatedSA,
  title={Thiophosphorylated substrate analogs are potent active site-directed inhibitors of protein-tyrosine phosphatases.},
  author={K. T. Hiriyanna and D A Baedke and Kwan Hyuck Baek and B A Forney and G J Kordiyak and Thomas S. Ingebritsen},
  journal={Analytical biochemistry},
  year={1994},
  volume={223 1},
  pages={51-8}
}
Thiophosphotyrosyl protein and peptide substrate analogs were found to be potent and specific protein-tyrosine phosphatase inhibitors with IC50s in the range of 0.2-30 microM. The analogs were based on highly reactive substrates and included thiophosphotyrosyl forms of reduced carboxamidomethylated and maleylated lysozyme and peptides based on tyrosine phosphorylation sites of lysozyme, alpha s2-casein, and platelet-derived growth factor receptor. These analogs inhibited protein-tyrosine… CONTINUE READING

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