SERMs and SARMs: Detection of their activities with yeast based bioassays

T.F.H. Bovee, M. Thevis, A.R.M. Hamers, A.A.C.M. Peijnenburg, M.W.F. Nielen, W.G.E.J. Schoonen

Research output: Contribution to journalArticleAcademicpeer-review

30 Citations (Scopus)

Abstract

Selective estrogen receptor modulators (SERMs) and selective androgen receptor modulators (SARMs) are compounds that activate their cognate receptor in particular target tissues without affecting other organs. Many of these compounds will find their use in therapeutic treatments. However, they also will have a high potential for misuse in veterinary practice and the sporting world. Here we demonstrate that yeast estrogen and androgen bioassays can be used to detect SERMs and SARMs, and are also useful screening tools to investigate their mode of action. Six steroidal 11ß-substituents of E2 (SERMs) and some arylpropionamide- and quinoline-based SARMs were tested. In addition, 7 compounds previously tested on AR agonism and determined as inactive in the yeast androgen bioassay, while QSAR modelling revealed strong binding to the human androgen receptor, are now shown to act as AR antagonists.
Original languageEnglish
Pages (from-to)85-92
JournalJournal of Steroid Biochemistry and Molecular Biology
Volume118
DOIs
Publication statusPublished - 2010

Keywords

  • androgen receptor modulator
  • advanced prostate-cancer
  • doping control purposes
  • in-vitro
  • bicalutamide
  • estrogen
  • binding
  • metabolism
  • membrane
  • blockade

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