Products/Services Used | Details | Operation |
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Peptide Synthesis | … Peptides and Phospho-Peptides were synthesized and purified using standard Fmoc chemistry by GenScript (Piscataway, NJ). Coupling of a tracer peptide to fluorescein isothiocyanate for a fluorescent polarization (FP) assay was also done by GenScript … | Get A Quote |
The polo-box domain (PBD) of PLK1 determines mitotic substrate recognition and subcellular localization. Compounds that target PLK1 selectively are required due to the tumor-suppressor roles of PLK3. A structure-activity analysis of the PBD phosphopeptide binding motif has identified potent peptides that delineate the determinants required for mimicry by nonpeptidic inhibitors and provide insights into the structural basis for the selectivity of inhibitors for the PLK1 PBD. Fragment-ligated inhibitory peptides (FLIPs) obtained through REPLACE have been optimized to enhance in vitro binding and a systematic analysis of selectivity for PLK1 vs PLK3 has been carried out for peptides and peptidomimetics. Furthermor... More