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. 2019 Feb 10;9(5):1021–1034. doi: 10.1016/j.apsb.2019.02.001

Figure 1.

Fig. 1

Inhibition of PLK1 PBD by MCC1019. (A) Inhibition of the binding of fluorescein-labeled phosphopeptides to PLK1, PLK2 or PLK3 PBDs by MCC1019 using a fluorescence polarization assay. The data are represented as mean ± SD of three independent experiments. (B) Thermophoresis binding curve of MCC1019 to the PLK1 and PLK1 PBD obtained by microscale thermopheresis. (C) Surface visualization of molecular docking of MCC1019 to the PLK1 PBD (PDB: 4X9R). (D) SeeSAR visualization of MCC1019 binding to human PLK1 (PDB: 4X9R): HYDE corona coloring is based on atomic affinity: green for favourable and red for unfavourable predicted affinities between atoms and amino acids. (E) Dose response curves of MCC1019 for different cancer cell lines obtained by cytotoxicity resazurin reduction assay, with westernblot analysis of PLK1 expression on each cell. The data are represented as mean ± SD of three independent experiments.