Recent Developments in Androgen Receptor Antagonists. Issue 11 (13th October 2015) - Ran, Fansheng
Abstract : The androgen receptor (AR), a ligand‐dependent transcription factor that regulates the expression of a series of downstream target genes after the binding of androgens, has been a target for the discovery of drugs used to treat prostate cancer. Prostate cancer always progresses to castration‐resistant prostate cancer after a period of androgen deprivation therapy. Thus, developing potent androgen receptor antagonists for the therapy of castration‐resistant prostate cancer possesses great significance. This review summarizes the preclinical development of androgen receptor antagonists, conventional androgen receptor antagonists that competitively bind to the ligand binding domain of the androgen receptor and coactivator antagonists of the androgen receptor, including both activation function‐2 antagonists and binding function‐3 antagonists. We hope that this review can help other researchers find new scaffolds and sites for the treatment of prostate cancer. Abstract : Prostate cancer always progresses to castration‐resistant prostate cancer after treatment with androgen receptor antagonists for a period of time. Combinational therapy with conventional antagonists and coactivator antagonists may provide novel therapeutic strategies to treat castration‐resistant prostate cancer in the near future.