Acute BRCAness Induction and AR Signaling Blockage through CDK12/7/9 Degradation Enhances PARP Inhibitor Sensitivity in Prostate Cancer
Fu Gui, Baishan Jiang, Jie Jiang, Zhixiang He, Takuya Tsujino, Tomoaki Takai, Seiji Arai, Celine Pana, Jens W. Köllermann, Gary Andrew Bradshaw, Robyn J. Eisert, Marian Kalocsay, Anne Fassl, Steven P. Balk, Adam Stuart Kibel, Jia Li
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.
Science Advances · Apr 23, 2025Peer-reviewedCancer Biology