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Interactions between androgen and estrogen receptors and the effects on their transactivational properties

V Panet-Raymond1, B Gottlieb, L K Beitel

  • 1Lady Davis Institute for Medical Research, Sir Mortimer B. Davis-Jewish General Hospital, 3755 Cote-Ste-Catherine Road, Quebec, H3T 1E2, Montreal, Canada.

Molecular and Cellular Endocrinology
|September 23, 2000
PubMed

Insights

Androgen receptor (AR) and estrogen receptor-alpha (ERalpha) directly interact, influencing their activity. This interaction between AR and ERalpha, but not ERbeta, provides biochemical insight into hormone interplay in endocrine tissues.

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Cellular Signaling

Background:

  • The physiological interplay between androgens and estrogens in endocrine tissues is established.
  • The specific biochemical mechanisms underlying this hormonal interplay require further definition.

Purpose of the Study:

  • To investigate the direct physical interaction between androgen receptor (AR) and estrogen receptors (ERalpha and ERbeta).
  • To determine the functional consequences of AR-ER interactions on transcriptional activity.

Main Methods:

  • Yeast and mammalian two-hybrid systems were employed to assess direct protein-protein interactions between AR and ERalpha/ERbeta.
  • DNA cotransfection studies using reporter gene constructs were performed to measure the functional impact of AR-ER interactions on transactivation.

Main Results:

  • Direct physical interaction was observed between the ligand-binding domain of ERalpha and the transactivational domain or full-length AR.
  • Estrogen receptor-beta (ERbeta) did not exhibit interaction with AR.
  • Coexpression of ERalpha with AR reduced AR transactivation by 35%, while coexpression of AR with ERalpha decreased ERalpha transactivation by 74%.
  • AR and ERbeta coexpression did not significantly alter AR or ERbeta transactivation.

Conclusions:

  • Specific domains of AR and ERalpha physically interact, establishing a direct molecular link.
  • These AR-ERalpha interactions lead to significant functional modulation of both receptors' transactivation capabilities.
  • The findings provide a biochemical basis for understanding the physiological interplay between androgens and estrogens.

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