Definition

An orally bioavailable inhibitor of polo-like kinase 4 (PLK4), with potential antineoplastic activity. Upon oral administration, PLK4 inhibitor RP-1664 selectively inhibits PLK4, which results in the disruption of mitosis and the induction of apoptosis. This inhibits the proliferation of tumor cells that overexpress PLK4 and/or tripartite motif-containing protein 37 (TRIM37). PLK4, a member of the polo family of serine/threonine kinases overexpressed in a variety of cancer cell types, plays a crucial role in the regulation of centriole duplication during the cell cycle. Tumors with a high level of the E3 ubiquitin-protein ligase TRIM37 rely on PLK4 for survival.