Fig. 3

A schematic diagram illustrating two distinct strategies for targeting Plk1. ATP-competitive analogs have been widely developed to inhibit the catalytic activity of Plk1, while PBD-binding antagonists are being developed to competitively inhibit the function of PBD. KD kinase domain, PBD polo-box domain. In the diagram, the PBD is shown to interact with a phosphorylated epitope on a substrate, and it tethers the cis-acting N-terminal KD in close proximity to its substrate. ATP adenosine triphosphate, ADP adenosine diphosphate