A cell-permeable allosteric inhibitor of PTP1B
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Protein tyrosine phosphatase 1B (PTP1B) has critical roles in cell signaling relevant to diabetes, obesity, and cancer. PTP1B inhibitor is a cell-permeable allosteric inhibitor of PTP1B (IC50s = 4 and 8 µM for 403 and 298 residue PTP1B forms, respectively). It binds reversibly and non-competitively, altering the conformation of the catalytic pocket. PTP1B inhibitor selectively increases the phosphorylation of the insulin receptor, insulin receptor substrate 1, and Akt, mimicking the action of insulin.
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