Identification of optimized Aurora Kinase A PROTACs with suitable PK properties for in vivo proof-of-concept studies (OPTIMAPK). Ghent University
Proteolysis targeting chimeras (PROTACs) are small molecule drugs able to selectively remove a disease-causing protein from cells and have emerged as a game-changing technology in drug discovery. We used this technology to induce the removal of Aurora Kinase A, a protein with crucial tumour growth-inducing functions in cancers such as leukemia, prostate cancer and neuroblastoma. We were able to identify a state-of-the-art PROTAC with very ...