Authors
Deborah S Mortensen, Surendra Nayak, Veronique Plantevin-Krenitsky, Evan J Horn, Joseph Meiring, Samantha Reiss, Kimberly Peacock, Jingjing Zhao, Xiaochu Ba, Stephen Norris, Matt Alexander, Matthew Correa, Dehua Huang, Jean-Francois Brazeau, John Sapienza, Lida Tehrani, Mark Nagy, Brandon Whitefield, Patrick Papa, Roy Harris, Virginia Grant, John D Norris, Massimo Ammirante, Emily Rychak, Suzanne E Wardell, Toshiya Tsuji, Courtney G Havens, Ken Liu, Joseph R Piccotti, Deepak Dalvie, Yang Tang, Nadia Guerrero, Lisa Sapinoso, Joshua Baughman, Brian E Cathers, Mark Rolfe, Lawrence G Hamann, Donald P McDonnell, Rama Krishna Narla, Joshua D Hansen, Shuichan Xu
Published in
Journal of medicinal chemistry. Jul 10, 2026. Epub Jul 10, 2026.
Abstract
Androgen receptor (AR) signaling is central to the progression of prostate cancer, including castration-resistant disease. Targeted protein degradation, particularly through heterobifunctional compounds, represents a significant advancement in eliminating disease-causing proteins beyond traditional inhibition. Here, we describe the medicinal chemistry discovery of BMS-986365, a novel dual-function AR degrader and an antagonist. BMS-986365 selectively and efficiently degrades both wild-type and clinically relevant mutant ARs while also antagonizing residual AR activity. This dual mechanism results in the robust inhibition of AR-driven pathways and prostate cancer cell growth. The development of BMS-986365 highlights the potential of targeted protein degradation strategies to overcome resistance and improve therapeutic outcomes in prostate cancer.
PMID:
42430428
Bibliographic data and abstract were imported from PubMed on 11 Jul 2026.
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