Recent advances in Liver X Receptor biology and chemistry

被引：26

作者：

Goodwin, Bryan J. ^{[1
]}

Zuercher, William J. ^{[1
]}

Collins, Jon L. ^{[1
]}

机构：

[1] GlaxoSmithKline Res & Dev Ltd, Res Triangle Pk, NC 27709 USA

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2008年 / 8卷 / 09期

关键词：

Liver X Receptors; LXR chemotypes; LXR crystal structure; LXR therapeutic indications;

D O I：

10.2174/156802608784535075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The Liver X Receptors LXR alpha and LXR beta are ligand-activated transcription factors that belong to the nuclear hormone receptor superfamily. Seminal studies with genetic and chemical tools were instrumental in the elucidation of cholesterol metabolism, gluconeogenesis, inflammation, and lipogenesis as signaling pathways that are controlled by the LXRs. First generation non-steroidal LXR agonists show beneficial effects in multiple animals models of human disease yet have not progressed in the clinic due to deleterious side effects in the liver. Numerous reports have appeared in the the recent literature that disclose new LXR signaling pathways and the identication of novel LXR chemotypes that may show improved therapeutic indices. This review will provide a brief historical perspective but will primarily focus on recent advances in LXR biology and chemistry.

引用

页码：781 / 791

页数：11

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