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Updated: Apr 1, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
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Recent Developments in Androgen Receptor Antagonists

Fansheng Ran1, Hualu Xing1, Yang Liu1

  • 1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong, P. R. China.

Archiv Der Pharmazie
|October 14, 2015
PubMed

Insights

This review covers androgen receptor (AR) antagonists for treating castration-resistant prostate cancer. It summarizes preclinical developments of AR antagonists, including conventional and coactivator types, to aid future drug discovery.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Androgen receptor (AR) is a key target in prostate cancer therapy.
  • Prostate cancer often progresses to castration-resistant prostate cancer (CRPC) despite androgen deprivation therapy.
  • Developing novel AR antagonists is crucial for effective CRPC treatment.

Purpose of the Study:

  • To review the preclinical development of androgen receptor antagonists.
  • To categorize AR antagonists into conventional and coactivator types.
  • To identify new therapeutic strategies for prostate cancer.

Main Methods:

  • Literature review of preclinical studies on AR antagonists.
  • Classification of AR antagonists based on their mechanism of action (ligand binding domain competitive inhibitors, coactivator antagonists).
  • Analysis of activation function-2 and binding function-3 antagonists.

Main Results:

  • Summarized various classes of AR antagonists.
  • Highlighted conventional AR antagonists that compete for AR ligand binding.
  • Detailed coactivator antagonists, including AF-2 and BF-3 antagonists.

Conclusions:

  • Preclinical development of AR antagonists shows promise for CRPC treatment.
  • Understanding different antagonist classes can guide the discovery of new drug scaffolds.
  • Further research into novel AR antagonist sites is needed for improved prostate cancer therapies.
Keywords:
Activation function-2Androgen receptor antagonistBinding function-3Ligand binding domainProstate cancer

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