Schering Aktiengesellschaft

Bayer Schering Pharma Ag

Maik Obendorf

Siegmund Wolf

Jens Schroeder

Rene Meyer

In the method of determining hormonal effects of substances, a test substance is contacted with Ewing sarcoma protein (EWS) or a derivative of it and with an androgen receptor (NR) or a derivative of it; and the effect of the test substance on binding of EWS with the androgen receptor or its derivative or on ligand-induced activity of the androgen receptor is determined, preferably in a cellular system. A method for determining interference in the co-modulator mechanism between androgen receptor and EWS, which includes measurement of androgen receptor and EWS concentrations, is described. A method for identification and characterization of substances that influence the activity of a nuclear receptor, especially androgen receptor, using EWS or a derivative of it is disclosed.

Methods for determining hormonal effects of substances using Ewing sarcoma protein and androgen receptor

The method for testing of substances for hormonal effects, especially for androgenic or anti-androgenic effects, includes exposing cells transfected with two vectors to the substances, wherein one vector contains a DNA, which codes for a nuclear receptor protein, or a fragment thereof, especially a human nuclear receptor protein, or a fragment thereof, and the other vector contains a DNA, which codes for the HSRNAAM co-modulator, or a fragment thereof; and measuring transcription activity, which the nuclear receptor protein, or its fragment, activates or releases in the presence of the HSRNAAM co-modulator, or its fragment, and/or measuring the influence of the substance on the interaction between the nuclear receptor protein, or its fragment, and the HSRNAAM co-modulator, or its fragment, by protein-protein interaction or by protein-protein-DNA interaction. Also a method for determining interference in the co-modulation mechanism between androgen receptor protein and HSRNAAM co-modulator is described.

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Weimar, Germany

Maik Obendorf