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PTP1B Inhibitors Protein tyrosine phosphatase-1B (PTP1B) is a highly validated molecular target, which mediates insulin resistance in mammals. PTP1B dephosphorylates the insulin receptor (IR) thus blunting its ability to transduce signal upon insulin binding. Inhibitors of PTP1B would be expected to restore activity to the IR and thus would find therapeutic benefit in the treatment of diabetes. TransTech Pharma discovered multiple classes of compounds that are potent, competitive reversible inhibitors of PTP1B that have shown efficacy in a cell-based assay, possess oral bioavailability, and lower blood glucose in the obese/obese mouse and in the glucose challenged mouse. TransTech currently has TTP814 in preclinical development. |
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