Targeting Androgen/Estrogen Receptors Crosstalk in Cancer

Michalis V Karamouzis1, Kostas A Papavassiliou1, Christos Adamopoulos1

  • 1Molecular Oncology Unit, Department of Biological Chemistry, Medical School, National and Kapodistrian University of Athens, 11527 Athens, Greece.

Trends in Cancer
|July 26, 2017
PubMed

Insights

Estrogen receptors (ERα, ERβ) and androgen receptors (AR) play key roles in breast and prostate cancers. Understanding their crosstalk is crucial for developing effective targeted therapies.

Area of Science:

  • Endocrinology
  • Oncology
  • Molecular Biology

Background:

  • Estrogen receptors (ERα and ERβ) mediate estrogen actions, with distinct transcriptional activities.
  • Estrogen receptor beta (ERβ) and its isoforms are linked to endocrine treatment response in breast tumors.
  • Androgen receptor (AR) is vital for prostate and certain breast cancer progression, influenced by coregulators.

Purpose of the Study:

  • To review the molecular mechanisms of androgen/estrogen receptor crosstalk.
  • To discuss therapeutic targeting strategies for hormone-driven breast and prostate cancers.

Main Methods:

  • Genomic landscaping of ERα and ERβ binding sites.
  • Analysis of post-translational modifications, dimerization, and localization of ERβ.
  • Review of coregulator influence on AR and ER activity.

Main Results:

  • Genomic studies reveal differential ERα and ERβ transcriptional regulation.
  • ERβ modifications and localization are critical in prostate cancer.
  • Coregulators dynamically modulate AR and ER activity in tumorigenesis.

Conclusions:

  • Targeting the crosstalk between androgen and estrogen receptors offers potential therapeutic avenues.
  • Understanding receptor interactions is key to optimizing AR-directed treatments in breast and prostate cancer.

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