NCIt definition : An orally bioavailable, adenosine triphosphate (ATP) competitive inhibitor of polo-like
kinase 1 (PLK1; PLK-1; STPK13), with potential antineoplastic activity. Upon administration,
onvansertib selectively binds to and inhibits PLK1, which disrupts mitosis and induces
selective G2/M cell-cycle arrest followed by apoptosis in PLK1-overexpressing tumor
cells. PLK1, named after the polo gene of Drosophila melanogaster, is a serine/threonine
kinase that is crucial for the regulation of mitosis, and plays a key role in tumor
cell proliferation. PLK1 expression is upregulated in a variety of tumor cell types
and high expression is associated with increased aggressiveness and poor prognosis.;