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

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...

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Bibliographic Details
Published inTrends in pharmacological sciences (Regular ed.) Vol. 33; no. 7; pp. 394 - 404
Main Authors Jakobsson, Tomas, Treuter, Eckardt, Gustafsson, Jan-Åke, Steffensen, Knut R
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 01.07.2012
Subjects
Advanced Basic Science
Amino Acid Sequence
Animals
Cholesterol - analogs & derivatives
Cholesterol - chemistry
Cholesterol - pharmacology
Drug Design
Homeostasis - physiology
Humans
Liver X Receptors
Medicin och hälsovetenskap
Mice
Models, Molecular
Molecular Sequence Data
Molecular Targeted Therapy
Orphan Nuclear Receptors - agonists
Orphan Nuclear Receptors - chemistry
Orphan Nuclear Receptors - physiology
RNA, Messenger - biosynthesis
Transcription Factors - metabolism
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Summary: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.
Bibliography:ObjectType-Article-2
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ObjectType-Review-1
ISSN:0165-6147
1873-3735
1873-3735
DOI:10.1016/j.tips.2012.03.013