Acute BRCAness Induction and AR Signaling Blockage through CDK12/7/9 Degradation Enhances PARP Inhibitor Sensitivity in Prostate Cancer
F. Gui, B. Jiang, J. Jiang, Z. He, T. Tsujino, T. Takai, S. Arai, C. Pana, J. Koellermann, G. A. Bradshaw, R. Eisert, M. Kalocsay, A. Fassl, S. P. Balk, A. S. Kibel, L. Jia
This paper introduces BSJ-5-63, a PROTAC that degrades CDK12, CDK7, and CDK9, inducing BRCAness and blocking AR signaling to enhance PARP inhibitor sensitivity in prostate cancer.
bioRxiv · Jul 9, 2024 · PreprintCancer Biology