Recent Advances in Liver X Receptor Biology and Chemistry

Authors: Goodwin, Bryan J.; Zuercher, William J.; Collins, Jon L.

Source: Current Topics in Medicinal Chemistry, Volume 8, Number 9, June 2008 , pp. 781-791(11)

Publisher: Bentham Science Publishers

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Abstract:

The Liver X Receptors LXRα and LXRβ 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.

Keywords: Liver X receptors; LXR chemotypes; LXR crystal structure; LXR therapeutic indications

Document Type: Research article

DOI: http://dx.doi.org/10.2174/156802608784535075

Affiliations: 1: GlaxoSmithKline Research and Development, NTH-1510, Five Moore Drive, Research Triangle Park,North Carolina, 27709 USA.

Publication date: 2008-06-01