PLK1

PLK1 is the best-characterized Polo-like kinase and a master mitotic regulator in mammalian cells. Its N-terminal kinase domain phosphorylates substrates bearing primed phosphopeptides that are recognized by the C-terminal polo-box domain, creating a substrate-targeting switch. PLK1 drives centrosome maturation, bipolar spindle assembly, activation of the anaphase-promoting complex, and cytokinesis, and it is degraded in late mitosis. Expression is strictly cell-cycle-dependent, peaking in G2/M, and PLK1 is overexpressed in a wide range of tumors with poor prognosis. Numerous clinical inhibitors, including volasertib and onvansertib, have validated PLK1 as an anticancer target, making recombinant PLK1 a staple for kinase-screening assays.