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Antiandrogens: selective androgen receptor modulators.

Cor A Berrevoets1, Arzu Umar, Albert O Brinkmann

  • 1Department of Reproduction and Development, Erasmus University Medical Centre Rotterdam, PO Box 1738, DR-3000 Rotterdam, The Netherlands.

Molecular and Cellular Endocrinology
|February 8, 2003
PubMed
Summary

Antiandrogens are crucial for treating prostate cancer by blocking androgen receptor (AR) gene expression. However, certain mutations allow antiandrogens to activate the AR, potentially promoting cancer growth.

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Area of Science:

  • Molecular Endocrinology
  • Oncology
  • Pharmacology

Background:

  • Androgen receptor (AR) signaling drives prostate cancer progression.
  • Antiandrogens are standard treatments, inhibiting AR-mediated gene expression.
  • AR mutations can alter treatment response.

Purpose of the Study:

  • To investigate how AR mutations affect antiandrogen activity.
  • To understand the conformational changes induced by antiandrogens in mutant AR.
  • To explore the implications for prostate cancer therapy.

Main Methods:

  • Studied ligand-induced conformational changes in wild-type and mutant AR (Thr877Ala).
  • Assessed the recruitment of co-regulators (coactivators and corepressors) to AR.
  • Evaluated the transcriptional activity of antiandrogens (cyproterone acetate, hydroxyflutamide) on mutant AR.

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Main Results:

  • Antiandrogens induce distinct AR conformations compared to androgens.
  • The Thr877Ala mutation alters AR conformation in response to antiandrogens.
  • Cyproterone acetate and hydroxyflutamide act as agonists on the mutant AR, unlike on wild-type AR.

Conclusions:

  • AR mutations confer agonist activity to antiandrogens by mimicking androgen-induced conformations.
  • This mechanism may explain treatment resistance and disease progression in some prostate cancers.
  • Targeting mutant AR signaling represents a potential therapeutic strategy.