Increased expression of genes converting adrenal androgens to testosterone in androgen-independent prostate cancer

Cancer Res. 2006 Mar 1;66(5):2815-25. doi: 10.1158/0008-5472.CAN-05-4000.

Abstract

Androgen receptor (AR) plays a central role in prostate cancer, and most patients respond to androgen deprivation therapies, but they invariably relapse with a more aggressive prostate cancer that has been termed hormone refractory or androgen independent. To identify proteins that mediate this tumor progression, gene expression in 33 androgen-independent prostate cancer bone marrow metastases versus 22 laser capture-microdissected primary prostate cancers was compared using Affymetrix oligonucleotide microarrays. Multiple genes associated with aggressive behavior were increased in the androgen-independent metastatic tumors (MMP9, CKS2, LRRC15, WNT5A, EZH2, E2F3, SDC1, SKP2, and BIRC5), whereas a candidate tumor suppressor gene (KLF6) was decreased. Consistent with castrate androgen levels, androgen-regulated genes were reduced 2- to 3-fold in the androgen-independent tumors. Nonetheless, they were still major transcripts in these tumors, indicating that there was partial reactivation of AR transcriptional activity. This was associated with increased expression of AR (5.8-fold) and multiple genes mediating androgen metabolism (HSD3B2, AKR1C3, SRD5A1, AKR1C2, AKR1C1, and UGT2B15). The increase in aldo-keto reductase family 1, member C3 (AKR1C3), the prostatic enzyme that reduces adrenal androstenedione to testosterone, was confirmed by real-time reverse transcription-PCR and immunohistochemistry. These results indicate that enhanced intracellular conversion of adrenal androgens to testosterone and dihydrotestosterone is a mechanism by which prostate cancer cells adapt to androgen deprivation and suggest new therapeutic targets.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • 3-Hydroxysteroid Dehydrogenases / biosynthesis
  • 3-Hydroxysteroid Dehydrogenases / genetics
  • Aldo-Keto Reductase Family 1 Member C3
  • Androgens / metabolism*
  • Gene Expression Regulation, Neoplastic
  • Genes, Tumor Suppressor
  • Humans
  • Hydroxyprostaglandin Dehydrogenases / biosynthesis
  • Hydroxyprostaglandin Dehydrogenases / genetics
  • Hydroxysteroid Dehydrogenases / biosynthesis
  • Hydroxysteroid Dehydrogenases / genetics
  • Male
  • Neoplasms, Hormone-Dependent / genetics
  • Neoplasms, Hormone-Dependent / metabolism
  • Prostatic Neoplasms / genetics*
  • Prostatic Neoplasms / metabolism*
  • Receptors, Androgen / biosynthesis
  • Receptors, Androgen / genetics
  • Reverse Transcriptase Polymerase Chain Reaction
  • Testosterone / biosynthesis*

Substances

  • Androgens
  • Receptors, Androgen
  • Testosterone
  • 3-Hydroxysteroid Dehydrogenases
  • Hydroxysteroid Dehydrogenases
  • Hydroxyprostaglandin Dehydrogenases
  • AKR1C2 protein, human
  • AKR1C3 protein, human
  • Aldo-Keto Reductase Family 1 Member C3