Development of Molecular Probes for Second-Site Screening and Design of Protein Tyrosine Phosphatase Inhibitors
Development of Molecular Probes for Second-Site Screening and Design of Protein Tyrosine Phosphatase Inhibitors
We report on the design, synthesis, and evaluation of a series of furanyl-salicyl-nitroxide derivatives as effective chemical probes for second-site screening against phosphotyrosine phosphatases (PTPs) using NMR-based techniques. The compounds have been tested against a panel of PTPs to assess their ability to inhibit a broad spectrum of these phosphatases. The utility of the derived compounds is illustrated with the phosphatase YopH, a bacterial toxin from Yersinia pestis. Novel chemical fragments were identified during an NMR-based screen for compounds that are capable of binding on the surface of YopH in regions adjacent the catalytic site in the presence of the spin-labeled compounds. Our data demonstrate the value of the derived chemical probes for NMR-based second-site screening in PTPs.
- Sanford Burnham Prebys Medical Discovery Institute United States
Models, Molecular, Magnetic Resonance Spectroscopy, Stereoisomerism, Salicylates, Cyclic N-Oxides, Structure-Activity Relationship, Catalytic Domain, Spin Labels, Protein Tyrosine Phosphatases, Furans, Bacterial Outer Membrane Proteins
Models, Molecular, Magnetic Resonance Spectroscopy, Stereoisomerism, Salicylates, Cyclic N-Oxides, Structure-Activity Relationship, Catalytic Domain, Spin Labels, Protein Tyrosine Phosphatases, Furans, Bacterial Outer Membrane Proteins
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