PLK1-PROTAC

PLK1-PROTAC is an experimental proteolysis-targeting chimera (PROTAC) designed to induce the degradation of Polo-like kinase 1 (PLK1), a key regulator of the cell cycle that is frequently overexpressed in various malignancies, including colorectal cancer (CRC). Unlike traditional small molecule inhibitors that only block kinase activity, this PROTAC leverages the ubiquitin-proteasome system to selectively degrade the PLK1 protein, potentially offering a more robust therapeutic effect and overcoming resistance mechanisms. Preclinical research presented at AACR 2026 demonstrated that PLK1-PROTAC significantly impairs CRC cell proliferation, migration, and invasion. Furthermore, in vivo studies in mouse models showed that PLK1-PROTAC, especially when used in combination with oxaliplatin, exerts enhanced suppression of tumor growth and may help overcome chemoresistance in advanced colorectal cancer.

Other names

PLK1-targeting PROTACPLK-1-targeting PROTACPLK 1-targeting PROTAC