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Non-Steroidal Steroid Receptor Modulators

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Abstract:

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 nonsteroidal ligands which have full or partial agonistic activity will be described for the following receptors: PR, GR, AR, LXR and FXR.

Keywords: androgen receptor; fxr; glucocorticoid receptor; lxr; non-steroidal; nuclear receptor modulators; progesterone receptor

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867053764671

Affiliations: N.V. Organon, Molenstraat 110, PO Box 20, 5340 BH Oss, The Netherlands.

Publication date: May 1, 2005

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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