Skip to main content
Article thumbnail
Location of Repository

Inhibition of androstenediol-dependent LNCaP tumour growth by 17α-ethynyl-5α-androstane-3α, 17β-diol (HE3235)

By R Trauger, E Corey, D Bell, S White, A Garsd, D Stickney, C Reading and J Frincke


Androst-5-ene-3β, 17β-diol (AED) is an adrenal hormone that has been reported to sustain prostate cancer growth after androgen deprivation therapy (ADT). LNCaP cells express a mutated androgen receptor that confers the ability to respond not only to androgen but also to oestrogen and adrenal hormones such as AED, and thus provide a cell line useful for identifying compounds capable of inhibiting AED-stimulated cell growth. We sought to determine whether structurally related steroids could inhibit AED-stimulated LNCaP cell growth in vitro and tumour growth in vivo. We report here the identification of a novel androstane steroid, HE3235 (17α-ethynyl-5α-androstan-3α, 17β-diol), with significant inhibitory activity for AED-stimulated LNCaP proliferation. This inhibitory activity is accompanied by an increase in the number of apoptotic cells. Animal studies have confirmed the cytoreductive activity of HE3235 on LNCaP tumours. The results suggest that this compound may be of clinical use in castration-resistant prostate cancer

Topics: Translational Therapeutics
Publisher: Nature Publishing Group
OAI identifier:
Provided by: PubMed Central

Suggested articles


  1. (1996). Control of LNCaP proliferation and differentiation: actions and interactions of androgens, 1alpha, 25-dihydroxycholecalciferol, all-trans retinoic acid, 9-cis retinoic acid, and phenylacetate. Prostate 28: 182–194
  2. (2003). Growth inhibition and differentiation in human prostate carcinoma cells induced by the vitamin D analog 1alpha, 24-dihydroxyvitamin D2. Prostate 55: 159–167 Cantor A
  3. (2007). Importance of the intracrine metabolism of adrenal androgens in androgendependent prostate cancer. Prostate Cancer Prostatic Dis 10(3): 301–306

To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.