Staff Publications

Staff Publications

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    'Staff publications' is the digital repository of Wageningen University & Research

    'Staff publications' contains references to publications authored by Wageningen University staff from 1976 onward.

    Publications authored by the staff of the Research Institutes are available from 1995 onwards.

    Full text documents are added when available. The database is updated daily and currently holds about 240,000 items, of which 72,000 in open access.

    We have a manual that explains all the features 

Record number 400121
Title SERMs and SARMs: Detection of their activities with yeast based bioassays
Author(s) Bovee, T.F.H.; Thevis, M.; Hamers, A.R.M.; Peijnenburg, A.A.C.M.; Nielen, M.W.F.; Schoonen, W.G.E.J.
Source Journal of Steroid Biochemistry and Molecular Biology 118 (2010). - ISSN 0960-0760 - p. 85 - 92.
Department(s) RIKILT - Business Unit Safety & Health
RIKILT - R&C Groeibevorderaars
Laboratory for Organic Chemistry
Publication type Refereed Article in a scientific journal
Publication year 2010
Keyword(s) androgen receptor modulator - advanced prostate-cancer - doping control purposes - in-vitro - bicalutamide - estrogen - binding - metabolism - membrane - blockade
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.
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