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Liver X receptor biology and pharmacology: new pathways, challenges and opportunities

Jakobsson, Tomas, Treuter, Eckardt, Gustafsson, Jan-Åke, Steffensen, Knut R.·2012·Trends in Pharmacological Sciences

Abstract

Nuclear receptors (NRs) are master regulators of transcriptional programs that integrate the homeostatic control of almost all biological processes. Their direct mode of ligand regulation and genome interaction is at the core of modern pharmacology. The two liver X receptors LXRα and LXRβ are among the emerging newer drug targets within the NR family. LXRs are best known as nuclear oxysterol receptors and physiological regulators of lipid and cholesterol metabolism that also act in an anti-inflammatory way. Because LXRs control diverse pathways in development, reproduction, metabolism, immunity and inflammation, they have potential as therapeutic targets for diseases as diverse as lipid disorders, atherosclerosis, chronic inflammation, autoimmunity, cancer and neurodegenerative diseases. Recent insights into LXR signaling suggest future targeting strategies aiming at increasing LXR subtype and pathway selectivity. This review discusses the current status of our understanding of LXR biology and pharmacology, with an emphasis on the molecular aspects of LXR signaling that constitute the potential of LXRs as drug targets.

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Metadata

Authors
Jakobsson, T., Treuter, E., Gustafsson, J.-Å., & Steffensen, K. R.
Venue
Trends in Pharmacological Sciences
Publisher
Elsevier BV
Published
2012-07
Volume
33
Issue
7
Pages
394-404
ISSN
0165-6147
Cited by
302
References
7
Language
en

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