Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
, 33 (7), 394-404

Liver X Receptor Biology and Pharmacology: New Pathways, Challenges and Opportunities


Liver X Receptor Biology and Pharmacology: New Pathways, Challenges and Opportunities

Tomas Jakobsson et al. Trends Pharmacol Sci.


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.

Similar articles

  • Targeting Liver X Receptors in Inflammation
    KR Steffensen et al. Expert Opin Ther Targets 17 (8), 977-90. PMID 23738533. - Review
    The new discoveries of LXR-regulated inflammatory pathways have ignited new promises for LXRs as drug targets. The broad physiological roles of LXRs involve a high risk o …
  • Action Mechanisms of Liver X Receptors
    C Gabbi et al. Biochem Biophys Res Commun 446 (3), 647-50. PMID 24300092. - Review
    The two Liver X Receptors, LXRα and LXRβ, are nuclear receptors belonging to the superfamily of ligand-activated transcription factors. They share more than 78% homology …
  • Identification of 5α, 6α-epoxycholesterol as a Novel Modulator of Liver X Receptor Activity
    TJ Berrodin et al. Mol Pharmacol 78 (6), 1046-58. PMID 20837678.
    The liver X receptors (LXRα and LXRβ) are members of the nuclear receptor superfamily that function as key transcriptional regulators of a number of biological processes, …
  • Regulation of Lipoprotein Lipase by the Oxysterol Receptors, LXRalpha and LXRbeta
    Y Zhang et al. J Biol Chem 276 (46), 43018-24. PMID 11562371.
    Lipoprotein lipase (LPL) is a key enzyme for lipoprotein metabolism and is responsible for hydrolysis of triglycerides in circulating lipoproteins, releasing free fatty a …
  • Liver X Receptors, Atherosclerosis and Inflammation
    DR Michael et al. Curr Atheroscler Rep 14 (3), 284-93. PMID 22419222. - Review
    Liver X receptors (LXRs) belong to the nuclear receptor superfamily of ligand-dependent transcription factors. LXRs are activated by oxysterols, metabolites of cholestero …
See all similar articles

Cited by 88 PubMed Central articles

See all "Cited by" articles

Publication types

LinkOut - more resources