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We report on the design and evaluation of novel cyclic peptides targeting the N‐terminal domain of the protein tyrosine phosphatase YopH from Yersinia. Cyclic peptides have been designed based on a short sequence from the protein SKAP‐HOM [DE(pY)DDPF (pY = phosphotyrosine)], and they all contain the motif DEZXDPfK (where Z is a phosphotyrosine or a non‐hydrolyzable phosphotyrosine mimetic, X is an...
We describe the use of a furanyl salicyl nitroxide derivative (‘spin‐labeled’ compound), as a paramagnetic phosphotyrosine mimetic, to carry out a second‐site screening by NMR against the PTPase YopH from Yersinia pestis. Using such a fragment‐based screening approach we identified several small molecules targeting YopH that bind at sites adjacent to the spin‐labeled compound. These second‐site fragments...
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