Androgen Receptor Variants and Castration-resistant Prostate Cancer: Looking Back and Looking Forward Takuma Uo, Cynthia Sprenger European Urology

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Androgen Receptor Variants and Castration-resistant Prostate Cancer: Looking Back and Looking Forward Takuma Uo, Cynthia Sprenger European Urology Volume 73, Issue 5, Pages 724-726 (May 2018) DOI: 10.1016/j.eururo.2017.12.020 Copyright © 2017 European Association of Urology Terms and Conditions

Fig. 1 Androgen receptor (AR) isoforms form homo- and heterodimers. Abiraterone limits the availability of dihydrotestosterone (DHT), while enzalutamide (Enza) antagonizes the ligand-binding domain (LBD) of AR, thus inhibiting the genomic actions of full-length AR (AR-FL). AR variants (AR-Vs) that retain the entire N-terminal domain and DNA-binding domain, may have nuclear localization and be constitutively active, while others may require liganded AR-FL or constitutively active AR-Vs to be localized in the nucleus, and thus exhibit “conditional” activities. The presence of multiple combinations of dimerization may diversify AR signaling, thereby contributing to resistance to current anti-AR therapies. European Urology 2018 73, 724-726DOI: (10.1016/j.eururo.2017.12.020) Copyright © 2017 European Association of Urology Terms and Conditions