Key clinical point: Standard of care for castration-resistant prostate cancer involves androgen receptor signaling inhibitors (ARSI), but this treatment is largely ineffective because of the development of ARSI drug resistance.
Major finding: Data suggest that AR function could be stopped biochemically with antagonists that target the ligand-binding domain and biophysically with cryo electron microscopy (Cryo-EM) but more research is needed.
Study details: The data come from a review of biochemical and biophysical approaches to blocking androgen receptor activity in castration-resistant prostate cancer.
Disclosures: The study was supported by the National Institutes of Health, and by multiple DoD Idea Development grants to study authors. Lead author Dr. Asangani had no financial conflicts to disclose.
Asangani IA et al. J Biol Chem. 2020 Dec 31. doi: 10.1074/jbc.REV120.012411.