Development of androgen receptor antagonists with promising activity in castration-resistant prostate cancer.
Androgen receptor (AR) continues to play a central role in prostate cancers that relapse after androgen deprivation therapy, but these tumors are refractory to available AR antagonists. In a recent issue of Science, Tran et al. describe an antagonist that prevents AR recruitment to chromatin and shows efficacy in relapsed prostate cancer.
Shen
Howard C
HC
Department of Medicine, Hematology-Oncology Division, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02115, USA.
Balk
Steven P
SP
D059002:Androgen Receptor Antagonists; D000728:Androgens; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001549:Benzamides; D002843:Chromatin / Q000378:metabolism; D006801:Humans; D008297:Male; D009364:Neoplasm Recurrence, Local; D009570:Nitriles; D009919:Orchiectomy; D010669:Phenylthiohydantoin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011944:Receptors, Androgen / Q000502:physiology*; D015398:Signal Transduction; D015533:Transcriptional Activation / Q000187:drug effects
D059002:Androgen Receptor Antagonists; D000728:Androgens; D000970:Antineoplastic Agents; D001549:Benzamides; D002843:Chromatin; D009570:Nitriles; D011944:Receptors, Androgen; D010669:Phenylthiohydantoin; C540278:enzalutamide