Journal: ChemMedChem

Article Title: Peptidomimetic Polo-Box targeted inhibitors that engage PLK1 in tumor cells and are selective against the PLK3 tumor suppressor.

doi: 10.1002/cmdc.202000137

Figure Lengend Snippet: In vitro binding activ ity for PLK PBD Peptides

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA); 41.4 nM PLK1 and 245 nM PLK3 were used per reaction.

Techniques: In Vitro, Binding Assay, Sequencing

Journal: ChemMedChem

Article Title: Peptidomimetic Polo-Box targeted inhibitors that engage PLK1 in tumor cells and are selective against the PLK3 tumor suppressor.

doi: 10.1002/cmdc.202000137

Figure Lengend Snippet: PLK PBD In vitro binding and cellular activity for optimized FLIP compounds.

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA); 41.4 nM PLK1 and 245 nM PLK3 were used per reaction.

Techniques: In Vitro, Binding Assay, Activity Assay, Sequencing

Journal: ChemMedChem

Article Title: Peptidomimetic Polo-Box targeted inhibitors that engage PLK1 in tumor cells and are selective against the PLK3 tumor suppressor.

doi: 10.1002/cmdc.202000137

Figure Lengend Snippet: Interactions of the Cdc25C phosphopeptide (yellow carbon atoms) with the PBD of both PLK1 (PDB ID: 3BZI) and PLK3 (homology model). PLK1 PBD residues are depicted with green carbon atoms and those of PLK3 are shown with orange carbons.

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA); 41.4 nM PLK1 and 245 nM PLK3 were used per reaction.

Techniques:

Journal: ChemMedChem

Article Title: Peptidomimetic Polo-Box targeted inhibitors that engage PLK1 in tumor cells and are selective against the PLK3 tumor suppressor.

doi: 10.1002/cmdc.202000137

Figure Lengend Snippet: Graph representing densitometry of the western blots of PLK1 and PLK3 across the dose range of the FLIPs listed.

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA); 41.4 nM PLK1 and 245 nM PLK3 were used per reaction.

Techniques: Western Blot

Journal: Molecular cancer therapeutics

Article Title: Targeting sub-cellular localization through the Polo-Box Domain: non-ATP competitive Inhibitors recapitulate a PLK1 phenotype

doi: 10.1158/1535-7163.MCT-12-0006-T

Figure Lengend Snippet: IC 50 values for PBD peptides derived from CDC25c and PBIP

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA) and 250 ng was used per reaction.

Techniques: Derivative Assay, Sequencing

Journal: Molecular cancer therapeutics

Article Title: Targeting sub-cellular localization through the Polo-Box Domain: non-ATP competitive Inhibitors recapitulate a PLK1 phenotype

doi: 10.1158/1535-7163.MCT-12-0006-T

Figure Lengend Snippet: PLK PBD In vitro binding and cellular activity for FLIP compounds (Ncap-S[pT]PNGL)

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA) and 250 ng was used per reaction.

Techniques: In Vitro, Binding Assay, Activity Assay

Journal: Molecular cancer therapeutics

Article Title: Targeting sub-cellular localization through the Polo-Box Domain: non-ATP competitive Inhibitors recapitulate a PLK1 phenotype

doi: 10.1158/1535-7163.MCT-12-0006-T

Figure Lengend Snippet: Treatment of HeLa cells with PBD inhibitors leads to reduced localization of PLK1 to the centrosomes. The Y-axis represents arbitrary fluorescent intensity units. Control represents fluorescence intensity data from untreated cells. QQ represents the data from cells treated with transfection reagent alone. The remainder represent data from cells transfected with the following peptides: 292 (LLCS[pT]PNGL), 5743 (Ac-PLHS[pT]A), 5781 (Ac-PLHS[pT]A), 5788 (3G1-S[pT]PNGL). Statistically significant decreases in fluorescent intensity were observed for 5743, 5781 and 5788.

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA) and 250 ng was used per reaction.

Techniques: Fluorescence, Transfection

Journal: Molecular cancer therapeutics

Article Title: Targeting sub-cellular localization through the Polo-Box Domain: non-ATP competitive Inhibitors recapitulate a PLK1 phenotype

doi: 10.1158/1535-7163.MCT-12-0006-T

Figure Lengend Snippet: Representative images from HeLa cells expressing GFP-H2B and immunostained for PLK1. (a) normal metaphase from an untreated cell, (b) aberrant prometaphase from a cell transfected with 5743, (c) aberrant, quadripolar metaphase from a cell transfected with 5743, (c) aberrant, tripolar metaphase from a cell transfected with 5788.

Article Snippet: The PLK1 PBD (367–603) and PLK3 PBD (335–646) proteins were obtained from BPS Bioscience Inc. (San Diego, CA) and 250 ng was used per reaction.

Techniques: Expressing, Transfection