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FKBP51 and FKBP52 regulate androgen receptor dimerization and proliferation in prostate cancer cells

Keisuke Maeda1, Makoto Habara1, Mitsuyasu Kawaguchi2

  • 1Department of Biochemistry, Joint Faculty of Veterinary Science, Yamaguchi University, Japan.

Molecular Oncology
|May 31, 2021
PubMed

Insights

Prostate cancer growth relies on the androgen receptor (AR). FKBP51 and FKBP52 proteins are crucial for AR signaling, and targeting them may inhibit cancer cell growth.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Prostate cancer progression is driven by the androgen receptor (AR).
  • FKBP51 and FKBP52 are immunophilins that modulate AR activity, but their exact roles are not fully understood.

Purpose of the Study:

  • To elucidate the mechanism by which FKBP51 and FKBP52 regulate androgen receptor (AR) signaling in prostate cancer.
  • To investigate the potential of FKBP51 and FKBP52 as therapeutic targets for prostate cancer.

Main Methods:

  • Depletion of FKBP51 or FKBP52 using specific techniques.
  • Assessing AR dimer formation, chromatin binding, and phosphorylation.
  • Evaluating the impact of FKBP51's isomerase activity on AR signaling and cancer cell proliferation.
  • Treating prostate cancer cells with FK506 and MJC13 inhibitors.
  • Correlating FKBP52 expression with clinical outcomes in prostate cancer patients.

Main Results:

  • Depleting FKBP51 or FKBP52 impaired AR dimer formation, chromatin binding, and phosphorylation, indicating defective AR signaling.
  • FKBP51's peptidyl-prolyl cis/trans isomerase activity is essential for AR dimer formation and prostate cancer cell growth.
  • Inhibitors FK506 and MJC13 blocked AR dimer formation in prostate cancer cells.
  • Higher FKBP52 expression correlated with increased prostate-specific antigen recurrence in patients.

Conclusions:

  • FKBP51 and FKBP52 play critical roles in AR signaling pathways essential for prostate cancer growth.
  • Targeting FKBP51 and FKBP52, potentially through small molecule inhibitors, represents a promising therapeutic strategy for prostate cancer.
Keywords:
immunophilinpeptidyl-prolyl cis/trans isomeraseprostate cancersteroid receptor

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