Sung-Eun Kim

TL;DR: The first K(M) optimization of a library of nitrophenylphosphate-containing substrates for generating an inhibitor lead against the Yersinia pestis outer protein phosphatase (YopH) is reported, with good YopH selectivity relative to a panel of phosphatases.

TL;DR: The described oxime-based library protocol provides detailed procedures for the linkage of aminooxy functionality with aldehyde building blocks that result in the generation of libraries of multidentate inhibitors.

TL;DR: Crystal structures of Tsg101 in complex with two structurally-modified PTAP-derived peptides define new regions of ligand interaction not previously identified with canonical peptide sequences, which could be highly useful in the design ofTsg101-binding antagonists.

TL;DR: In the first unambiguous demonstration of IzD interactions with a PTP other than PTP1B, it is shown by X-ray crystallography that the IZD motif binds within the catalytic site of the Yersinia pestis PTP YopH by similarly displacing a highly conserved water molecule.

TL;DR: This work represents the first successful example of the application of peptoid-peptide hybrids in the design of SH2 domain-binding antagonists, and could provide a foundation for further structural optimization of Shc SH2domain-binding peptide mimetics.