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Curr Med Chem. 2005;12(9):1017-75.

Non-steroidal steroid receptor modulators.

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N.V. Organon, Medicinal Chemistry Department, P.O. Box 20, 5340 BH, Oss, The Netherlands.


The last ten years much attention has been focused on the finding of non-steroidal ligands for steroidal nuclear receptors for reasons such as diminishing cross-reactivity to eliminate side effect profiles, changing physicochemical properties which might cause different tissue distribution profiles and altering binding modes which influence the binding of cofactors. Compounds with a selective functionality profile are referred to as selective nuclear receptor modulators (e.g., SARMs or SPRMs). In the following paragraphs non-steroidal ligands which have full or partial agonistic activity will be described for the following receptors: PR, GR, AR, LXR and FXR.

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