Non-steroidal steroid receptor modulators

被引：35

作者：

Buijsman, RC ^{[1
]}

Hermkens, PHH ^{[1
]}

van Rijn, RD ^{[1
]}

Stock, HT ^{[1
]}

Teerhuis, NM ^{[1
]}

机构：

[1] NV Organon, Dept Med Chem, NL-5340 BH Oss, Netherlands

来源：

CURRENT MEDICINAL CHEMISTRY | 2005年 / 12卷 / 09期

关键词：

non-steroidal; nuclear receptor modulators; progesterone receptor; androgen receptor; glucocorticoid receptor; FXR; LXR;

D O I：

10.2174/0929867053764671

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1017 / 1075

页数：59

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