A designed cell-permeable aptamer-based corepressor peptide is highly specific for the androgen receptor and inhibits prostate cancer cell growth in a vector-free mode

Endocrinology. 2011 Jun;152(6):2174-83. doi: 10.1210/en.2011-0149. Epub 2011 Apr 12.

Abstract

The repression of the androgen receptor (AR) activity is a major objective to inhibit prostate cancer growth. One underlying mechanism for efficient hormone therapy is based on corepressors that inactivate the AR. In line with this, castration-resistant prostate cancer is associated with malfunction or reduced corepressor action. To overcome this, the overexpression of endogenous corepressors, however, affects many other transcription factors. Therefore, an AR-specific corepressor could be of advantage. Using a yeast peptide aptamer two-hybrid screen with the full-length human AR, we identified a short amino acid-stretch that binds specifically to the human AR in yeast and in mammalian cells and not to the closely related progesterone or glucocorticoid receptors. Furthermore, fused to a silencing domain, this aptamer-based corepressor (AB-CoR) exhibits corepressor activity by inhibiting both the AR-mediated transactivation and expression of the AR target gene PSA. Furthermore, stable expression of the AB-CoR inhibits growth of human LNCaP prostate cancer cells. Moreover, we generated a cell-permeable AB-CoR by fusing a protein transduction domain to establish a vector-free transport system. Treatment of LNCaP cells with the bacterially expressed and affinity-purified cell-permeable AB-CoR peptide resulted in a significant inhibition of both AR-mediated transactivation and prostate cancer cell proliferation. Thus, generation of a novel AR-specific aptamer-based corepressor may present a vector-free inhibition of AR-dependent prostate cancer growth as a novel approach.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aptamers, Peptide / chemical synthesis
  • Aptamers, Peptide / genetics
  • Aptamers, Peptide / metabolism
  • Aptamers, Peptide / pharmacokinetics*
  • Cell Line, Tumor
  • Cell Proliferation*
  • Co-Repressor Proteins / chemical synthesis
  • Co-Repressor Proteins / genetics
  • Co-Repressor Proteins / metabolism*
  • Co-Repressor Proteins / pharmacokinetics
  • Down-Regulation* / drug effects
  • Humans
  • Male
  • Permeability
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / genetics
  • Prostatic Neoplasms / metabolism*
  • Prostatic Neoplasms / physiopathology*
  • Protein Binding
  • Receptors, Androgen / genetics
  • Receptors, Androgen / metabolism*
  • Species Specificity
  • Transcriptional Activation / drug effects

Substances

  • Aptamers, Peptide
  • Co-Repressor Proteins
  • Receptors, Androgen