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

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...

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Bibliographic Details
Published in:The Journal of steroid biochemistry and molecular biology 2010, Vol.118 (1), p.85-92
Main Authors: Bovee, Toine F.H., Thevis, Mario, Hamers, Astrid R.M., Peijnenburg, Ad A.C.M., Nielen, Michel W.F., Schoonen, Willem G.E.J.
Format: Article
Language:English
Subjects:
advanced prostate-cancer
Agonists
Androgen Antagonists - analysis
Androgen Receptor Antagonists
androgen receptor modulator
Androgenic activity
Androgens - analysis
Animals
Antagonists
bicalutamide
binding
Biological and medical sciences
Biological Assay - methods
blockade
CHO Cells
Cricetinae
Cricetulus
doping control purposes
Estradiol - analogs & derivatives
Estradiol - analysis
estrogen
Estrogen Receptor alpha - agonists
Estrogen Receptor alpha - antagonists & inhibitors
Estrogen Receptor alpha - genetics
Estrogenic activity
Fundamental and applied biological sciences. Psychology
Green Fluorescent Proteins - genetics
Humans
In vitro bioassays
in-vitro
membrane
Metabolism
Molecular Structure
Receptors, Androgen - genetics
Selective Estrogen Receptor Modulators - analysis
Substance Abuse Detection - methods
Transcriptional Activation - genetics
Transfection
Vertebrates: endocrinology
Vertebrates: reproduction
Yeasts - genetics
Yeasts - metabolism
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Summary: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.
ISSN:0960-0760
1879-1220
DOI:10.1016/j.jsbmb.2009.10.007