NCIt definition : The fumarate form of onvansertib, 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.;
Semantic type(s)