Identification and Validation of a Potent Type II Inhibitor of Inactive Polo‐like Kinase 1

Abstract

Virtual screening using a homology model of human polo-like kinase 1 (Plk1) in an inactive conformation led to the identification of a selective Plk1 inhibitor that decreases proliferation and induces apoptosis. This suggests that type II Plk1 inhibitors may be considered for the development of cancer therapeutics.