Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 9, Pages 2137-2143Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm061481l
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Funding
- NIAID NIH HHS [AI055789, P01 AI055789-050006, P01 AI055789, AI058123, R21 AI058123-01, R21 AI058123] Funding Source: Medline
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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.
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