Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer

Oncogene. 2008 Dec 4;27(57):7201-11. doi: 10.1038/onc.2008.320. Epub 2008 Sep 15.

Abstract

Proteolysis targeting chimeric molecules (Protacs) target proteins for destruction by exploiting the ubiquitin-dependent proteolytic system of eukaryotic cells. We designed two Protacs that contain the peptide 'degron' from hypoxia-inducible factor-1alpha, which binds to the Von-Hippel-Lindau (VHL) E3 ubiquitin ligase complex, linked to either dihydroxytestosterone that targets the androgen receptor (AR; Protac-A), or linked to estradiol (E2) that targets the estrogen receptor-alpha (ERalpha; Protac-B). We hypothesized that these Protacs would recruit hormone receptors to the VHL E3 ligase complex, resulting in the degradation of receptors, and decreased proliferation of hormone-dependent cell lines. Treatment of estrogen-dependent breast cancer cells with Protac-B induced the degradation of ERalpha in a proteasome-dependent manner. Protac-B inhibited the proliferation of ERalpha-dependent breast cancer cells by inducing G(1) arrest, inhibition of retinoblastoma phosphorylation and decreasing expression of cyclin D1, progesterone receptors A and B. Protac-B treatment did not affect the proliferation of estrogen-independent breast cancer cells that lacked ERalpha expression. Similarly, Protac-A treatment of androgen-dependent prostate cancer cells induced G(1) arrest but did not affect cells that do not express AR. Our results suggest that Protacs specifically inhibit the proliferation of hormone-dependent breast and prostate cancer cells through degradation of the ERalpha and AR, respectively.

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

  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / chemistry
  • Blotting, Western
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dihydrotestosterone / administration & dosage
  • Dihydrotestosterone / metabolism
  • Drug Delivery Systems / methods*
  • Estradiol / administration & dosage
  • Estradiol / metabolism
  • Estrogen Receptor alpha / drug effects
  • Estrogen Receptor alpha / metabolism
  • Female
  • Flow Cytometry
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / administration & dosage
  • Hypoxia-Inducible Factor 1, alpha Subunit / chemistry
  • Male
  • Neoplasms, Hormone-Dependent / drug therapy
  • Neoplasms, Hormone-Dependent / metabolism
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism
  • Proteasome Endopeptidase Complex / drug effects
  • Receptors, Androgen / drug effects
  • Receptors, Androgen / metabolism
  • Receptors, Steroid / drug effects*
  • Receptors, Steroid / metabolism
  • Recombinant Fusion Proteins / administration & dosage
  • Recombinant Fusion Proteins / chemistry
  • Ubiquitination / physiology*

Substances

  • Antineoplastic Agents
  • Estrogen Receptor alpha
  • HIF1A protein, human
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Receptors, Androgen
  • Receptors, Steroid
  • Recombinant Fusion Proteins
  • Dihydrotestosterone
  • Estradiol
  • Proteasome Endopeptidase Complex