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

Authors
Journal
The Journal of Steroid Biochemistry and Molecular Biology
0960-0760
Publisher
Elsevier
Publication Date
Volume
118
Identifiers
DOI: 10.1016/j.jsbmb.2009.10.007
Keywords
  • Agonists
  • Antagonists
  • In Vitrobioassays
  • Androgenic Activity
  • Estrogenic Activity
  • Metabolism
Disciplines
  • Medicine

Abstract

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 11β-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.

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