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A) Inhibition of the protein tyrosine phosphatase PTP1B by the pentafluorophosphato‐phenylalanines 3 and 12, respectively, was 25‐fold and 30‐fold stronger than of the classical phosphono‐difluormethyl phenylalanine 1 and was further enhanced in peptide mimetics 15 and 16. B) Docking of 3 suggested the preferred binding pose in the phosphotyrosine binding pocket of PTP1B.
