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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| Published in | Trends in pharmacological sciences (Regular ed.) Vol. 33; no. 7; pp. 394 - 404 |
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| Main Authors | , , , |
| Format | Journal Article |
| Language | English |
| Published |
England
Elsevier Ltd
01.07.2012
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| Subjects | |
| Online Access | Get full text |
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| 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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| AbstractList | 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. |
| Author | Jakobsson, Tomas Gustafsson, Jan-Åke Steffensen, Knut R Treuter, Eckardt |
| Author_xml | – sequence: 1 fullname: Jakobsson, Tomas – sequence: 2 fullname: Treuter, Eckardt – sequence: 3 fullname: Gustafsson, Jan-Åke – sequence: 4 fullname: Steffensen, Knut R |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/22541735$$D View this record in MEDLINE/PubMed http://kipublications.ki.se/Default.aspx?queryparsed=id:124952550$$DView record from Swedish Publication Index |
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| SubjectTerms | 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 |
| Title | Liver X receptor biology and pharmacology: new pathways, challenges and opportunities |
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