NCIt definition : An inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.
Upon administration, prexasertib selectively binds to chk1, thereby preventing activity
of chk1 and abrogating the repair of damaged DNA. This may lead to an accumulation
of damaged DNA and may promote genomic instability and apoptosis. Prexasertib may
potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance
to chemotherapeutic agents. Chk1, a serine/threonine kinase, mediates cell cycle checkpoint
control and is essential for DNA repair and plays a key role in resistance to chemotherapeutic
agents.;